Gw-501516 is a PPAR receptor agonist invented by Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. Gw-501516 was originally developed to treat obesity, diabetes, lipid strain, and cardiovascular diseases. Those who run blood work when using gw-501516 will notice that their cholesterol levels improve substantially.
PPAR receptor agonists are drugs that stimulate the expression of genes involved in the metabolism of glucose and fatty acids. There are three different PPAR isoforms:
• Alpha (α)
• Beta/Delta (β/ δ)
• Gamma (γ)
PPAR-alpha activation increases the expression of lipoprotein lipase and apolipoprotein A-V (apoA-V) and decreases the expression of apoC-III in the liver. This decreases LDL particles (bad cholesterol), decreases blood triglycerides levels and liberates fatty acids, allowing them to be oxidized (burned). In addition, PPAR-alpha activation increases hepatic apoA-I andapoA-II, which increasing HDL levels (good cholesterol). In summary, PPAR-alpha activation increases fat loss and improves cholesterol levels by lowering LDL levels, decreasing blood triglycerides and increasing HDL levels.
Note: LDL stands for low-density lipoprotein and is often referred to as bad cholesterol. HDL
stands for high-density lipoprotein and if often referred to as good cholesterol.
Note: A lipase is an enzyme that helps break down fats into glycerol and fatty acids.
The exact actions of PPAR-beta/delta in humans are still being researched. Animal studies show that PPAR-beta/delta activation decreases adipose tissue (body fat). Most researchers speculate that PPAR-beta/delta acts similarly to PPAR-alpha but has more specific actions in skeletal muscle, in both humans and animals.
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Activation of PPAR-gamma will increase the transcription of genes and enzymes involved in insulin sensitivity and decrease their activity in adipogenesis (fat cell creation) and the inflammatory process. Obesity and insulin resistance suppresses PPAR-gamma activation. Activation of PPAR-gamma could theoretically cure type 2 diabetes. The anti-diabetic drug thiazolidinediones have been successfully used to treat type-2 diabetes in human clinical trials through its role in activating PPAR-gamma, though hepatoxicity and risk of congestive heart failure discontinued the research on the drug.
Side effects are rare with Gw-501516. Since Gw-501516 is non-hormonal, there is no need to worry about post cycle therapy or hormone suppression. The recommended dose for both men and women is 10-20 milligrams (mg) per day. The half-life of gw-501516 is 20-24 hours, meaning that a once per day dose is all that is needed.
“20mg is my favorite GW-501516 dosage. I feel like it’s totally safe as long as it’s cycled. I prefer not to use it while bulking. Only while cutting. I feel like Gw-501516 sort of ‘flips a genetic switch’ that makes you more like an endurance athlete. I think it’s incredible while fasting, or when following a ketogenic or low carbohydrate diet. It’s also helpful in keeping energy levels high on low carb days when carb cycling. It’s very synergistic with other fat burners and I think it’s very helpful in preparing for a bodybuilding competition to keep energy and stamina up.
I typically recommend 20mg/day for both men and women. Unless a woman is less than 110 pounds, then I would tell her to use the only 10mg. I don’t think GW-501516 loses its effectiveness but I think being on it for longer periods of time increases risks. I personally feel comfortable using it 5 days on/ 2 days off, 2 weeks on/1 week off, or 1 month on/1 week off.”
-DR. TONY HUGE
“I don’t feel that GW-501516 is necessarily good for muscle gain, but it’s very good for weight loss and cardio benefits. I notice a rapid improvement in cardio when taking it. It’s good for people getting ready for bodybuilding contests, endurance athletes, and fighters. It supports weight loss. Benefits start as low as 10mg/day. I’ve experimented with dosages as high as 50mg/day but noticed no benefits going past 30mg/day.
I found the injectable version (called cardiolone) superior to the oral version. If you suspend GW-50516 in water, it’s slow action. If you suspend it in solution, it is fast-acting.”
Sr-9009 is a Rev-ErbA agonist developed by Professor Thomas Burris from The Scripps Research Institute. His initial findings were published in the journal of Natural Medicine showing that sr-9009 supplementation significantly increased weight loss, stamina, and endurance while lowering blood cholesterol, inflammation, and the risk for developing heart disease. Professor Burris’ study found that the sr-9009 supplementation led to a 50% increased metabolic activity in skeletal muscle, even when exercise was restricted. The sedentary animals developed muscles just like an athlete who had been training. The sr-9009 supplementation also caused the resting metabolic rate to increase, even in the absence of exercise.
Sr-9009 supplementation sets off a host of processes in the body by activating the Rev-Erb protein. In particular, sr-9009 increases mitochondria production in muscle cells, increasing metabolism, endurance and strength. Rats give sr-9009 experienced a 50% increment in their running speed. By also enhancing the metabolic rate of the individual, sr-9009 stimulates lipolysis and fat loss.
Sr-9009 may also offer other therapeutic benefits. Recent studies have revealed that daily sr9009 supplementation reduced plasma triglycerides by 12%, total cholesterol by 47%, plasma non-esterified fatty acids by 23%, plasma glucose by 19%, plasma insulins level by 35%, and pro-inflammatory cytokines by 72%.
Sr-9009 provides a lot of the same benefits as Gw-501516. In fact, the two are often stacked
together. The main difference between the two compounds is their half-lives. Gw-501516 has
a half-life of 24 hours whereas sr-9009 has a half-life of only 4 hours. The short half-life of sr9009 makes it optimal to supplement immediately before workouts. Sr-9009 is fat-soluble
so you want to take it with food, such as your pre-workout meal.
The recommended dosage is the same for men and women. If you are using sr-9009 by itself, you will want to take 10mg 3 times per day, spread out as much as possible. The easiest way would be to take 10mg at breakfast, lunch and dinner. If you are stacking sr-9009 and Gw501516, then you would take 20mg of Gw-501516 with breakfast and 10mg of sr-9009 with your pre-workout meal.
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“I haven’t had a chance to do too many experiments with SR-9009 yet but I did inject 50mg and got blood work done the next day. It massively improved my cholesterol. It’s hard to say if it can be attributed solely to the SR-9009 but it seems to have the potential to repair cholesterol side effects from steroids. I will be conducting more sr-9009 experiments in the near future. Stay tuned.
One side note – I’m worried that the oral form is not absorbable.”
– DR. TONY HUGE
“I really like it. I don’t like the oral version. The oral version has only a 2-3% bioavailability. I saw the most dramatic improvements in cardio with injectable SR-9009 then any other SARM. It helped preserve my muscle mass when fasting and doing fight training better then Gw-501516. SR-9009 increased the number of mitochondria and fixes broken mitochondria. An increase in mitochondria in muscle tissue has a direct relationship to increasing strength, endurance and muscle size.
The oral version is useless. The dosages needed would cause stomach distress. I’ve experimented with injectable sr-9009 dosages as high as 50mg/day. 10 to 25mg/day is the dosage I recommend for the average person.”
– COACH TREVOR
Mk-677 is a growth hormone secretagogue originally developed by Reverse Pharmacology. A secretagogue is a substance that causes another substance to be secreted. So in this case, mk677 signals the pituitary gland to secrete growth hormone. Mk-677 could be compared to secretagogue peptides like GHRP-6 or Ipamorelin, only it doesn’t require injections. Mk-677 was originally developed for the treatment of elderly patients to combat muscle wasting, obesity and osteoporosis. Although commonly referred and sold as a Selective Androgen Receptor Modulator (SARM), Mk-677 is actually not a SARM and is non-hormonal. As a result, Mk-677 does not affect natural testosterone production or the Hypothalamus-Pituitary-Testes-Axis (HPTA). This means that no post cycle therapy (PCT) is needed after Mk-677 usage and that Mk-677 can be safely included in PCTs and bridges between steroid cycles.
MK-677 WORKS VIA 4 MAIN MECHANISMS:
1. Increasing GHRH (growth hormone-releasing hormone).
2. Amplifying GHRH signaling in somatotrophs of the anterior pituitary gland.
3. Reducing somatostatin release (somatostatin turns off GH release).
4. Inhibiting of somatostatin receptor signaling.
In an Mk-677 trial that studied its effects on catabolic states, a daily dosage of 25mgs was given to healthy young men subjected to short-term diet-induced nitrogen wasting. After 7 days of this dose, the subjects showed a sustained increase in serum concentration of IGF1 and Growth Hormone. In addition, nitrogen wasting was reversed.
Trials testing the effects of Mk-677 on fighting obesity showed an increase in lean body mass. This study gave subjects 25mgs of Mk-677 per day for 8 weeks. The subjects saw an increase in basal metabolic rate, an increase in lean muscle mass, and an increase in serum levels of GH, IGF-1 and IGF-1 binding protein-3.
A study done for the treatment of osteoporosis and bone mineral density showed increases in bone mineral density. Other possible benefits of Mk-677 are improved sleep, improved complexion, increase in energy levels, increase nitrogen retention, increase strength and an improved sense of well-being. In addition, some studies also suggest that an increased immune system response was caused by Mk-677< meaning it boosts the immune system to a degree.
Human clinical trials on Mk-677 have been done with dosages ranging from 10-50mg per day. The trials found that although HGH release was no higher at 50mg/day then 10mg/day, an increase in IGF-1 was seen as dosages increased. This suggests that for general health and fat burning, a daily dosage of 10mg/day is sufficient to improve HGH levels and see results. However, to maximize the muscle-building effects of Mk-677, you should consider increasing your dosage up to a dosage of 50mg/day. As a general guideline, most users find a sweet spot at a dosage around 25mg per day.
Mk-677 has a half-life of 24 hours meaning that a once per day dosage is all that is required. The time of day you take Mk-677 is dependent on your goals. If your primary goal is fat loss, you should take Mk-677 first thing in the morning on an empty stomach to maximize fat oxidation. If your primary goal is muscle building, you should take Mk-677 before bed to maximize recovery and sleep. If your primary goal is recomposition (building muscle and losing fat at the same time), you should take half of your daily dosage before breakfast and half before bed each day.
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“MK-677 is the single most dangerous compound to the pharmaceutical companies profits because of its medical and performance-enhancing benefits. I predict that every informed person on anti-aging will use this compound or one of its successors. My only issue with MK-677 is the side effect of increased hunger. Personally, I already have too much hunger and suppressing my appetite is the goal – not increasing it. On the other hand, I’ve created many great bodybuilders using MK-677 because their limiting factor was eating enough food.
MK-677 does the same thing for men and women; increase lean muscle mass, improve recovery, promote fat loss, improve sleep, and increased appetite. After chronic prolonged use, common side effects can include day time lethargy, water retention, and tightness in the hands/wrists.
I didn’t see any additional benefit going above 30mg/day, but I saw a significant difference in benefits increasing my dosage from 10 to 20mg. I recommend people start at 10mg and increase their daily dosage up to 30mg if we want the more extreme benefits.
I think MK-677 replaces growth hormones completely for 90% of people. It doesn’t have to be cycled but the side effects of water retention and fatigue can accumulate over time, so take breaks as needed. I’ve known people who have taken it 6 months straight with no side effects and only continued benefits. I also know people who have taken it on and off for 7 years with no side effects beyond what was already mentioned.
I take it if I need to shred fat very fast and am using appetite suppressants or if I am trying to extreme bulk. I notice that it seems to improve my digestion, and speed of digestion. I prefer to take it at night before going to sleep so I can sleep through most of the hunger increase.”
– DR. TONY HUGE
“You won’t get much muscle-building from MK-677, but it will help hold onto mass and rejuvenate cells. With exogenous growth hormone – it’s the growth factor that causes muscle building, mainly IGF and MGF.
High dosages of MK-677 can cause stomach distress like Crohn’s. Once you get those symptoms, stop using it. It’s that ghrelin increase that’s causing it.
The problem with HGH secretagogue peptides is that they cause growth hormone bleeding. The bleed effect causes more side effects. MK-677 is superior because it sends HGH pulses throughout the day.
I’ve experimented with dosages up to 50mg/day. I didn’t notice much benefit going past 30mg/day. 10mg/day is the lowest dosage I started to see benefits. I noticed a significant increase in benefits increasing my dosage from 10mg/day to 20mg/day. I didn’t see much increase in benefits going from 20mg/day to 30mg/day.
I find that if I take a low dosage before bed it helps improve sleep. 10mg before bed is my sweet spot.”
– COACH TREVOR
D. OSTARINE (MK-2866)
Ostarine (MK-2866), also known as Ostabolic or Enobosarm was originally developed by GTX Pharmaceuticals to prevent muscle loss in people suffering from muscle-wasting conditions such as HIV and cancer.
GTX pharmaceuticals presented the results of a phase2 clinical trial evaluating Ostarine (MK2866) in patients with cancer-induced muscle loss (also known as cancer cachexia) at the Endocrine Society Annual Meeting, held in Washington 2009. In this study 159 cancer patients with cell lung cancer, colorectal cancer, non-Hodgkins lymphoma, chronic lymphocytic leukemia or breast cancer were randomized. Participants received a placebo, 1mg or 3mg Ostarine daily for 16 weeks. Patients were allowed to receive standard chemotherapy during the trial. Ostarine treatment led to statistically significant increases in lean body mass (LBM) and improvement in muscle performance in both the 1mg and 3mg cohorts. The primary endpoint of LBM was measured by a dual-energy x-ray absorptiometry (DEXA) scan. Ostarine demonstrated significant increases in LBM compared to baseline with average increases of 1.3kg and 1.5kg of LBM at the end of the 16-week trial, in the 1mg and 3mg groups respectively. The study also met the secondary endpoint of muscle function as measured by a 12-step stair climbing test measuring speed and calculating power, with each Ostarine treatment group demonstrating a statistically significant decrease in time to completion and an increase in the power exerted.
In clinical studies, Ostarine has consistently demonstrated increases in LBM and better physical function across several populations, along with a lower hazard ratio for survival in cancer patients. Full results from these studies will soon be published and will guide the development of future anabolic trials. While Ostarine was initially trialed at 0.1 mg, 0.3 mg, and 1 mg per day, dosages as high as 9 mg and 18 mg per day have been studied and were generally well tolerated by both men and women in a less commonly known phase II clinical trial.
Lean gains upwards of 5 – 10 pounds are typical among recreational users, with average dosages ranging from 12.5 – 25 mg per day in 8-12-week cycles.
Using Ostarine in A Steroid Cycle Post Cycle Therapy (PCT)
More and more recreational steroid users are including Ostarine in their Post Cycle Therapy. As a SARM, Ostarine selectively binds to the androgen receptors in muscle tissues. Ostarine continues activating androgen receptors while the PCT drugs Nolvadex and Clomid bring natural testosterone production back to normal. This continued activation prevents loss of muscle mass or strength during the PCT.
However, research shows that higher doses of Ostarine can cause HPTA suppression so you wouldn’t want to use too high of an Ostarine dosage in your PCT. However, the suppression isn’t too much of an issue because when you use Ostarine in conjunction with a SERM like Nolvadex (tamoxifen) or Clomid (clomiphene), the stimulation of the pituitary and hypothalamus from the Nolvadex/Clomid offsets the mild suppression from the Ostarine. In other words, Nolvadex and Clomid get your endogenous testosterone levels back to normal while Ostarine offers the therapeutic benefits of increased androgen receptor activity.
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“Ostarine was originally my favorite SARM because it did everything that I was hoping SARMS would do – increase strength and performance, improve recovery, build muscle, maintain muscle while dieting and give my muscles a dry hard look. However, I no longer use Ostarine very much because it’s very mild. It’s a great compound for beginners and intermediates but advanced users won’t see much benefit.
Women – 5mg per day or 5mg every other day, up to 10mg per day seems to have the most benefits with the least amount of side effects. I do know professional female athletes that use up to 30mg/day. But they often start to get swelling of the clitoris and an extreme sex drive at that dosage.
Men – in my early days of using Ostarine, I used 20mg/day to maintain muscle mass after a steroid cycle. At 10mg/day I started losing size. I noticed a big difference between 10 and 20mg. I really liked a daily 20mg dosage because I felt like I wasn’t experiencing any symptoms of low testosterone and in fact, my testosterone levels were actually recovering. I’ve taken up to 100mg/day. I didn’t notice any additional benefits taking dosages higher than 50mg/day. I think it plateaus at around 50mg/day.
I don’t have too much to say about Ostarine because I really don’t use it much. It’s more beneficial for beginner users and females.
Side note – An older female friend of mine with osteoporosis found huge therapeutic benefits from supplementing with Ostarine at 10mg/day.”
– DR. TONY HUGE
“I’m not a big fan of oral Ostarine but the injectable version could be very good. There is a lot of clinical information on injectable Ostarine. Lots of research using only 1-2mg/day with impressive results. I’m going to start experimenting with the injectable form. I am not sure about dosage recommendations because I haven’t used it yet.”
– COACH TREVOR
S-4 was studied in 120 ovariectomized rats (a female rat whose ovaries have been removed) for 120 days. The study found that treatment with S4 (S-4) was beneficial to maintain cortical bone content and whole-body bone mineral density (BMD) measured by DEXA scan. The S4 treatment also decreased body fat and increased body strength in these animals. It was also revealed that S-4 provides the unique potential to prevent bone resorption, increase skeletal muscle mass and promote bone anabolism, making it a possible new alternative treatment for osteoporosis and sarcopenia . To date, there are no clinical human studies with S-4. S-4 has a half-life of 4-6 hours and is prized as a weight loss and muscle boosting supplement in the fitness community.
Dosages of 25 – 100 mg per day are commonly used in a recreational context for muscle building purposes. There is no established therapeutic dosage of S4. Typically, users report more favorable outcomes splitting their daily dosage up into increments throughout the day to maintain stable blood serum concentration levels to account for S-4’s short 4-hour half-life. Anecdotally, S4 is reported to exhibit diminishing returns at dosages above 100 mg per day, with 50 mg commonly being referred to as “the sweet spot” dosage. Vision side effects are reported to occur in a significant number of users at dosages above 50 mg per day.
These dosages were determined by recreational users based upon personal experimentation and anecdotal experiences and are not indicative of correct or incorrect use.
Side Effects from S-4
Users may experience a suppression in luteinizing hormone (LH) and follicle-stimulating hormones (FSH) from S-4 usage. LH and FSH promote the production of reproductive hormones in men and women, and suppression could suppress normal estrogen/testosterone levels. However, it is unknown if and how much S-4 would actually suppress testosterone/estrogen production in humans. S-4 suppressed LH and FSH in castrated rats but had no effect in normal male rats.
Besides suppression, the most frequent user-reported side effect is visual issues such as seeing a yellow tint and difficulty adjusting to night vision. The S-4 molecule binds to the retina in the eye which causes a yellow tint to be seen. This generally occurs at night, especially when switching from a dark to lightened area. The side effect is not serious and will disappear immediately after the drug’s usage has been discontinued.
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“More men’s physique competitors have won competitions using only S4 than any other compound. It appears to be an adequate replacement for steroids in amateur physique divisions.
I personally don’t like it because even though the vision side effects are mild and temporary, I can’t afford any vision compromise because I’m constantly on my phone. It appears that the visual side effects and benefits are directly related to the dosage and duration of the cycle. Men seem to get great benefits from longer cycles at 50mg/day, or short cycles at 75-100mg/day. We also have had a lot of female competitors who have won physique competitions using only 25-50mg/day. This is surprisingly close to a man’s dosage, but they experienced no virilization side effects.
S4 gives a dry hard look to the muscles and maintains performance while dieting. I defiantly recommend cycling off because of the vision side effect. I personally like running a higher dosage for a short period of time before side effects accumulate.”
– DR. TONY HUGE
“I experienced vision side effects from oral S4. Even low dosages caused vision side effects. I’m not a fan of oral S4, especially at high dosages.
I have gone up to 150mg/day with injectable S4 with no vision side effects. It really dried out and hardened my physiques. My veins came out like crazy. Similar results to Winstrol. I recommended dosages of 50-100mg/day for men. At low dosages, it’s great for women. I recommend dosages of 10-25md/day for women. Women start to get side effects at dosages about 50mg/day.
S4 has a short half-life so it’s something you would to add into a stack instead of using it as the primary drug of choice.”
– COACH TREVOR
LGD-4033, also known as Ligandrol, is a SARM discovered by Ligand Pharmaceuticals and currently under licensed development by Viking Therapeutics. There has been a lot of research into the efficacy of LGD-4033, but very little published research. Ligandrol has exhibited desirable in vivo efficacy on skeletal muscle and bone measurements in animal models of disease. There is only one published study on the effects of LGD-4033 in humans. In 2013, Bhasia et al. conducted a rigorous 3-week placebo-controlled study of 76 healthy men aged 21 – 50 years old. During this study, participants were randomly assigned to be given a placebo, 0,1, .0,3 or 1mg of LGD-4033 for 21 days. There was a dose-dependent increase in lean body mass. There was also a dose-dependent increase in strength as measured by stair climbing speed and power. Adverse effects were not noted . The sample size was small, as the study’s primary aim was to establish safety and tolerability, rather than efficacy. As such, the 3-week study duration was not designed to demonstrate maximal effects on muscle mass and strength. Therefore, larger and longer studies are needed to access the efficacy of LGD-4033.
Dosages of 10mg per day for 8 to 12 weeks are commonly used in a recreational context for muscle building purposes. There is no established therapeutic dosage.
Side Effects from LGD-4033
LGD-4033 showed a dose-dependent suppression of total testosterone from baseline when given to healthy men aged 21-50 for 21 days. Upon discontinuation of LGD-4033, testosterone levels returned to normal by day 56.
It’s impossible to determine how long it would take for testosterone levels to return to normal after using LGD-4033 for an 8 to 12-week cycle. Anecdotal evidence shows the LGD4033 is one of the more suppressive SARMS, suggesting that a post cycle therapy is needed after using LGD-4033.
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“LGD is the second most effective SARM that we have used on professional bodybuilders. We still have not found the upper limit of what it’s capable of. I have seen bodybuilders who plateaued using steroids that switched to LGD and started making gains again.
For the oral dosage, one of the most impressive transformations I’ve seen used 120mg/ day oral. For the injectable, we have used 50mg/day on many professional bodybuilders to put on muscle. The injectable version is even more effective, and we can get a lot more effective with fewer side effects. The main side effect we get from high dosages of LGD is water retention and fatigue. Both of those side effects appear to be mitigated by using the injectable version.
One of the most impressive female transformations was a female taking 5mg of oral LGD EOD and within 2 weeks she had gained more muscle then she wanted. She hasn’t taken it since. The muscle gains appear to be permanent.”
– DR. TONY HUGE
“LGD is the SARM that woke me up into realizing that SARMS works. I was very skeptical of SARMS until trying LGD. It’s one of the best mass gainers I’ve ever used. Some water weight but no bloat. Mostly intracellular water inside the muscle tissue. The effects are similar to nandrolone like deca; increases in strength, joint relief, and helps with weight endurance. However, it kills cardio endurance.
I would compare the results of LGD as similar to a test/deca stack, but without the bloat.
Oral LGD works well. For women, it’s one of the best SARMS for size. I recommend 5-10mg/ day for women, but I don’t recommend they take it daily. Only 4-5 days per week. For men, I recommend 10-50mg/day every day.
The injectable version gives less androgenic side effects and less HPTA shut down. For women, I always recommend injectable LGD over oral. I typically recommend 10mg every Monday of an extended-release form of injectable LGD, called Magnalone XR.”
– COACH TREVOR
RAD-140 was developed by Radius Pharmaceuticals in the late 2000s as a potential therapeutic aid to prevent muscle wasting in terminally ill patients. It’s currently being researched as a therapeutic aid for breast cancer patients. The first phase clinical trials were conducted in 2017 and more are expected to follow.
RAD-140 has excellent pharmacokinetic properties and is a potent anabolic, as its anabolic-androgenic ratio is 90:1. RAD-140 is a potent androgen receptor (AR) agonist in breast cancer cells with a distinct mechanism of action, including the AR-mediated repression of estrogen receptor1 (ESR1). Phase 1 clinical trials found that RAD-140 inhibited the growth of multiple breast cancer patient-derived xenograft models in isolation. These preclinical data present support for further investigation of RAD-140 in breast cancer patients. The phase 1 clinical trials also showed that RAD-140 increased muscular weight without affecting the prostate. In addition, it lowered lipids (LDL, HDL, triglycerides), without elevation of liver enzymes.
In the fitness community, RAD-140 is seen as one of the latest additions to the lineup of SARMs. The increases in LBM and fat loss are highly appreciated. Recommended dosages of RAD-140 vary from 20- 30 mg once daily and it is used in cycles of 12-14 weeks duration. Because RAD140 does not interact with the aromatase enzyme and is not liver toxic, no adverse effects are claimed. The half-life of RAD-140 is 12-18 hours.
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“RAD140 is able to make the muscles denser and more defined, without increasing body weight. It seems like a great compound for athletes who are trying to increase performance without adding body weight. That’s why RAD140 is a favorite among MMA fighters.
I’ve also noticed that RAD140 has a nootropic benefit of focus and energy. I like to recommend RAD140 if a man says he’s having a hard time finding the motivation to workout. It helps increase motivation to work out and train hard.
I’ve found the side effect of anger and irritability can start to occur at dosages higher than 20mg/day. That being said, the benefits also keep increasing as you increase dosages up to 50mg/day. The highest dosage I ever used was 50mg/day and within 48 hours, there were extremely noticeable differences in the mirror. My muscles looked hard as granite and veins were popping everywhere.
Females – I haven’t seen any side effects in women, but I haven’t experimented with high
dosages. Females should use 5mg/day.”
– DR. TONY HUGE
“RAD140 is very expensive and very commonly faked because of the cost. I never experienced any side effects when using RAD140, other than the aggression side effects Dr. Tony Huge already mentioned.
RAD140 is kind of like the trenbolone of SARMS. It’s similar to s23. S23 leans you out a little bit more whereas RAD140 gives you a bit more strength.
I feel that it’s safe for both men and women. Women can start to get emasculating side effects at 15mg/day. I recommend 5-10mg/day for women and 20mg/day for men.
It’s a good SARM for anyone looking for strength, recomposition, aggression, mass, performance, muscle, and fat loss.”
– COACH TREVOR
YK11 is one of the newest SARMS to be developed. Due to its infancy, Yk11 has never passed the preclinical development stage and has never been tested on animals or humans. YK-11 is a steroidal selective androgen receptor modulator (SARM) and myostatin inhibitor that was popularized because of its potential to induct supraphysiological levels of follistatin expression.
Myostatin is a type of myokine protein that is the main genetic component that regulates muscle growth potential. Theoretically, YK11 would increases levels of follistatin, a unique type of protein found in the muscle cells which binds to and inhibits the actions of myostatin in the body. More follistatin equals less myostatin, and less myostatin means more muscle. In vitro cellular studies conducted on YK11 confirm that it has an anabolic effect on muscle tissue which is mediated through androgen receptor activation and induction of Follistatin expression. It is a very interesting compound that may have some very promising applications we have yet to learn about.
YK11 is classified as a SARM because it has selective activation of the androgen receptor, but it has a chemical structure very similar to DHT (dihydrotestosterone). The term SARM is applied relatively loosely in this context. Personally, I would classify YK11 as a hybrid of a steroid and a SARM.
While there is a decent amount of anecdotal information to reference due to its popularity in the bodybuilding community, the data itself is fairly limited, as only a minority of individuals are logging their blood work consistently, and even fewer are getting extensive testing done to establish exactly what effects YK11 had on their body. The majority of YK11 users are reporting impressive increases in muscle growth, strength gains, improvements in body composition, with temporary suppression of natural testosterone production being the most common obvious side effect. With the exception of hair loss, reports of other side effects from YK11 are typically less prevalent than with the more mainstream very suppressive SARMs, and this may be due to its close resemblance to DHT.
10 mg per day is the most common YK11 dosage used in a performance-enhancing context. Some users report using daily dosages as high as 30 mg per day and experiencing substantial gains in muscle mass with little to no negative side effects. Based on what we know, it would probably be unwise for a woman to use YK11 as it is a DHT derivative and has exhibited noticeable androgenic effects in men. The half-life of YK11 is unknown, so splitting the total daily dosage up into several micro-doses per day would likely yield better outcomes with more stable blood serum concentrations.
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YK11 features a methyl ester which inhibits its hepatic metabolism. This makes it very orally bioavailable. The drawback of orally active methylated steroids is that they are liver toxic. The chemical structure and anecdotal reports suggest that YK11 exhibits at least some level of hepatotoxicity (liver toxicity). Recreational users should use an over the counter liver support supplement while using YK-11, and users should not exceed 8 weeks.
“The highest dosage I ever used was 100mg of injectable YK-11 and 50mg of oral YK-11. I noticed extremely fast muscle growth. It was a similar feeling to taking a very high dosage of Anadrol. It seems to plateau very quickly. I recommend using a very high dosage for only a couple of days. Typically, a 5-day blast. What’s interesting is that I notice that after the 5 days, I keep making gains even though I stopped taking the YK-11, which makes me hypothesize that YK-11 helps re-sensitize the androgen receptors.
The YK-11 muscle gains are so extreme that we never felt the need to give it to women because women already gained more muscle then they wanted off of LGD.
We don’t know if it’s better to use a low dosage for a long period of time or a high dosage for a short period of time. We will be conducting more experiments in the future.”
– DR. TONY HUGE
“I’m very excited about YK11. It’s not a SARM. It’s not a steroid. It’s kind of like a weird hybrid of the two. It partly binds to the androgen receptor so other drugs can’t bind to it, which increases the affinity of the androgen receptor for other drugs, therefore increasing androgen receptor sensitivity. It also lowers myostatin by increasing follistatin. It’s methylated but anecdotal evidence shows no liver toxicity.
The oral version works great. It has a very short half-life. They use it as a pre-workout in Kuwait. I got even better results from the injectable version. It’s the most extreme thing I ever took. The injectable version you only need to inject once per day.
Women should stay away from the oral form. I recommend a dosage of 2-5 mg/day for a woman. Men can use either the oral or injectable form. I recommend 10-50mg/day for men.”
– COACH TREVOR
S23 is undoubtedly one of the strongest SARMs in development right now. S23 is currently under development for potential use as a male hormonal contraceptive.
It is still in the preclinical stage of development, meaning it has only been tested on animals, not humans.
S23 was created by modifying the structure of an older and less efficacious SARM called C-6 by changing the para-nitro group of C-6 to a cyano group. Pharmacokinetic studies showed that C-6 is 76% orally bioavailable, and by swapping the para-nitro group for a cyano group, S23 is able to achieve 96% oral bioavailability. This means that S23 can be administered orally, as opposed to requiring injections to achieve maximal blood serum concentration levels, which is obviously advantageous when it comes to ease of use and application.
The preclinical data revealed that S23 is the most suppressive SARM in development and resulted in infertility in all rats treated. Expectedly, this raised interest in its potential clinical applications as a form of male birth control.
S23 has become increasingly popular in the recreational bodybuilding community for its potent muscle building and body recomposition effects. Recreational users are quick to label S23 as a more potent alternative to S4 (S-4), without the night vision side effect. S23 has also shown to decrease the prostate size in studies, which is the opposite of a very common negative side effect of anabolic steroids (enlargement of the prostate). This data is commonly misinterpreted though, as all SARMs will prevent prostate hypertrophy in a dose-dependent manner, and this is specifically referred to in the study.
Dosages of 10 – 30 mg per day are commonly used in a recreational context for muscle building purposes. There is no established therapeutic dosage of S23. Anecdotally, S23 is reported to show diminishing returns at dosages above 30 mg per day. The mean terminal half-life of S23 in rats is 11.9 hours. The half-life of S23 in humans is unknown and would require a clinical study to determine it.
Androgen Receptor Binding Affinity
S23 has a very high binding affinity for the androgen receptor (AR) with a Ki of ~1.7 nM. Ki is a dissociation equilibrium constant defined kinetically as the ratio of rate constants koff/kon for the binding of the substrate to the androgen receptor. In lay man’s terms, the lower the Ki value, the higher the binding affinity for the androgen receptor. To put this in perspective, RAD-140 (RAD140) has a Ki value of 7 nM. S23 has a binding affinity over four times higher than RAD140, which was already considered impressive.
The binding affinity of Testosterone and DHT remains unclear as each study seems to render significantly different values but testosterone has a Ki value of roughly 40 nM. The only SARM in development that is reported to have a formidable binding affinity to S23 is LGD-4033, which has a Ki of ∼1 nM. However, due to the poor oral bioavailability of LGD4033, oral S23 will be much more potent when compared mg to mg.
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“S23 gives very similar results to trenbolone. I notice that if I use too high of a dosage of S23, my metabolism goes so fast that I start to lose weight because I can’t eat enough. With S23, it’s important to match the dosage to the number of calories eaten. With oral, I’ve gone up to 100mg/day. With injectable, I’ve gone up to 50mg/day. The benefits of 50mg S23 injectable were similar to 100mg oral. 5-10 mg/day is the dosage I recommend for women.
With oral, I’ve gone up to 100mg/day. With injectable, I’ve gone up to 50mg/day. The benefits of 50mg S23 injectable were similar to 100mg oral. 5-10 mg/day is the dosage I recommend for women.
I recommend cycling S23 because it is so suppressive of natural testosterone production. I notice that I experience testicular atrophy as I go up in dosage. When this side effect occurs, I use HCG to bring my testicles back to normal size.”
– DR. TONY HUGE
“S23 was the second SARM I experimented using high dosages with. S23 gives very similar results to the steroid trenbolone; incredible fat loss, mental energy, focus, and strength. My training was great when using S23. I noticed a great performance benefit.
S23 is my favorite SARM for women. Women get extreme results in both fat loss and muscle. I recommend 5-10mg/day for women.
For men, I recommend 20-40mg/day. I’ve personally experimented with dosages as high as
120mg/day. I noticed the benefits started to taper off around 80-100mg/day.”
– COACH TREVOR