RAD140 (TESTOLONE) DESCRIPTION
RAD140 (Testolone) is a potent, oral bioavailable, research nonsteroidal nonsteroidal androgen receptor modulator (SARM) devoloped as a future replacement for exogenous Testosterone replacement therapy (TRT) by Radius Health, Inc. Current RAD140 research focuses on the potential benefits of increasing muscle mass, fighting muscle wasting, skeletal wasting (osteoporosis), breast cancer and protecting brain cells. RAD140 Testolone has the chemical formula C20H16ClN5O2 and a molecular mass of 393.83 g mol−1.
THE RAD140 ANDROGEN RECEPTOR HAS PERFECT Affinity
RAD140 showed excellent affinity for the androgen receptor (Ki = 7 nM versus 29 nM for testosterone and 10 nM for dihydrotestosterone (DHT)) as well as good selectivity over other steroid hormone nuclear receptors, the closest off target receptor being the progesterone receptor (IC50 = 750 nM). vs 0.2 nM for progesterone). In vitro functional androgen agonist activity was confirmed in the C2C12 osteoblast differentiation assay, showing an EC50 of 0.1 nM (DHT = 0.05 nM).
AD140 EFFECTIVELY Stimulates MUSCLE MASS GROWTH
A clinical study published in 2011 examined the anabolic androgenic effect of RAD140 in young primates, male cynomolgous monkeys. Animal body weight results for 28 days of dosing with RAD140 at 0.01 mg/kg, 0.1 mg/kg, and 1 mg/kg are shown in the figure below:
In this study, mean weight gain was achieved only at the 0.1 mg/kg dose over the 28-day dose. A similar result was obtained in the 1.0 mg/kg dose group.
NEUROPROTECTIVE EFFECTS OF RAD140
A scientific study published in 2014 investigated the neuroprotective effects of rad140 in cultured rat neurons and male rat brain. Neuroprotection is an important neural action of endogenous androgens related to neural health and resilience against neurodegenerative diseases.
In cultured hippocampal neurons, RAD140 was as effective as testosterone in reducing cell death induced by apoptotic insults. Mechanistically, RAD140 neuroprotection was dependent on MAPK signaling, evidenced by upregulation of ERK phosphorylation and inhibition of protection by the MAPK kinase inhibitor U0126. More importantly, RAD140 was also neuroprotective in vivo using the rat kainate lesion model.
In experiments with gonadectomized, adult male rats, RAD140 has been shown to exhibit peripheral tissue-specific androgen action largely spared prostate, neural activity as shown by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of excitoxin kainate. These new findings demonstrate the first preclinical efficacy of a SARM in neuroprotective actions related to Alzheimer’s disease and related neurodegenerative diseases.
RAD140 (TESTOLONE) AND BODYBUILDING
Similar to anabolic steroids, RAD140 effectively stimulates the growth of muscle mass. However, its safety profile is significantly better compared to steroids. RAD140 has significantly fewer dangerous and unwanted side effects, and the potential health risks that anabolic steroid use can cause are many times lower. Therefore, RAD140 is also used (abuse) by bodybuilders, athletes and people who are trying to gain muscle figure, who want to achieve similar results when using steroids, but also want to eliminate / minimize possible unwanted side effects. We emphasize that RAD140 is not an approved nutritional supplement or stimulant for athletes: RAD140 is an experimental substance still under investigation, its long-term effects are not yet fully known and more research is needed. Note that the RAD140, like all our other products, is sold for scientific and research clinical use only.
RAD140 AND DOPING
While RAD140 is not illegal, it is illegal in professional sports. WADA (World Anti-Doping Agency) banned all Selective androgen receptor modulators (including RAD140) as early as 2008.
POSSIBLE BENEFITS OF RAD140 SCIENTIFICALLY RESEARCHED
Significant and selective anabolic effect on muscles and bones, without strong androgenic side effects on other organs
It has strong neuroprotective effects, may be effective in preventing Alzheimer’s disease and related neurodegenerative disorders
Has the potential to fight breast cancer
May help treat serious diseases associated with muscle wasting
May help preserve brain cells and their proper function
May help treat osteoporosis
Helps build and maintain muscle mass
May help reduce excess fat
ADVANTAGES OF RAD140 OVER ANABOLIC STEROIDS
RAD140 (Testolone) is selective and primarily intended for movement in muscles and bones. Due to this selectivity, it does not cause strong androgenic negative effects on other organs, unlike anabolic steroids.
Similar to anabolic steroids, RAD140 can help achieve significant muscle gains, but has significantly fewer dangerous and unwanted side effects, and the potential health risks that steroid use can cause are many times lower than that:
RAD140 does not convert to Estrogen or DHT
RAD140 does not cause significant retention of water and salts
RAD140 does not cause increased Cortisol levels
RAD140 does not cause prostate enlargement
RAD140 does not cause kidney disease
RAD140 does not cause acne and oily skin
RAD140 does not cause swollen face
RAD140 does not cause aggression, explosiveness
RAD140 is extremely effective when administered orally (no injection required)
Benefits of the RAD 150
Rad 150 offers a variety of benefits due to its high rate of absorption, stability, and half-life of 48 hours. At the same time, it has little to no side effects, especially when taken as recommended. This is discussed later in this article. Below are the many benefits that rad 150 offers to improve your performance as well as your physique.
It doesn’t increase aggression.
It doesn’t cause baldness.
It increases sexual performance and libido.
It has no effect on lipid metabolism.
It promotes muscle growth.
It has no androgenic effect.
Rad 150 ensures rapid muscle regeneration.
It is excellent for bulking cycles.
It has fast muscle recovery.
It’s a safer alternative.
It gives faster results.
Rad 150 has no harmful effects on the liver.
It has an extended half-life.
It has no side effects if taken properly.
It is very stable and has a high absorption rate.
As the scientific community adjusts to moving forward without LGD-4033, synthetic chemists are increasingly re-evaluating how to push the frontiers of SARM development to maximize potency, biodistribution, half-life, and tissue selectivity, while simultaneously Minimize off-target/side effects. The most cutting edge research SARMs under development are those that are rationally designed using the cumulative pharmacological knowledge gained from over 30 years of androgen research, rather than being discovered through screening or stupid luck, which typified SARMs development in the early days.
Please note that RAD-150 (TLB-150) was not developed by Radius Health, Inc. While the official name is TLB-150, it was dubbed RAD-150 due to its structural similarity to RAD-140, its parent compound.
RAD-150 belongs to a class of compounds called “Anabolic Esters” due to esterification during chemical synthesis. Historically, testosterone esterification has been pursued to allow for more stable serum testosterone levels. Now, synthetic chemists are applying these findings to SARMs research and development to achieve a similar goal: more stable and durable SARM serum levels.
OSTARINE (MK-2866) DESCRIPTION
Ostarine (also marked as MK-2866, Enobosarm and GTx-024) is an oral, nonsteroidal, and Selective androgen receptor modulator (SARM), developed for the treatment of conditions such as muscle wasting and osteoporosis (a health condition that weakens bones). In a phase 2a study, Ostarine has been shown to increase lean body mass, decrease fat mass, and improve modest homeostatic model evaluation (HOMA), a measure of insulin sensitivity. It is the best and best SARM clinically tested to date. Ostarine has the chemical formula C19H14F3N333, molecular mass 389.33 g.mol−1 and a long elimination half-life of 24 hours.
OSTARINE HISTORY AND DEVELOPMENT
Ostarine GTx, Inc. Developed for the treatment of conditions such as muscle wasting and osteoporosis. The company invested approximately $35 million in its development.
In August 2011, a double-blind, placebo-controlled phase II trial focused on older men and postmenopausal women. In this study, Ostarine showed statistically significant improvements in total lean body mass and physical function without androgenic negative side effects (usually occurring with steroid therapy).
In August 2013, GTx announced that Ostarine had failed in two Phase III clinical trials to treat wasting in people with lung cancer. Officials have also indicated that it plans to maintain Ostarine’s approval in Europe.
In 2016, GTx began Phase II trials to see if Ostarine was effective for treating stress urinary incontinence in women, but these trials failed to reach the primary endpoint in the ASTRID test in 2018.
OSTARINE ASSISTS TO GET SIGNIFICANT MUSCLE GAINS
A 12-week double-blind, placebo-controlled phase II clinical trial was conducted in 2006 to evaluate Ostarine in 120 healthy elderly men (>60 years) and postmenopausal women. The primary endpoint is total lean body mass as assessed by dual energy X-ray absorption, and the secondary endpoints include physical function, body weight, insulin resistance, and safety. Ostarine treatment resulted in statistically significant dose-dependent increases in total lean body mass (P < 0.001, 3 mg vs. placebo) and clinically significant. There were also significant improvements in physical function (P = 0.013, 3 mg vs. placebo) and insulin resistance (P = 0.013, 3 mg vs. placebo). The incidence of adverse events was similar between treatment groups. Ostarine showed a dose-dependent improvement in total lean body mass and physical function and was well tolerated. This study concluded that Ostarine may be useful in the prevention and treatment of muscle wasting associated with cancer and other chronic diseases.
A clinical study conducted in 2007-2008 examined the effects of Ostarine on muscle wasting and physical function in cancer patients. 159 patients were analyzed for safety (placebo, n=52; Ostarine 1 mg, n=53; Ostarine 3 mg, n=54). The valuable efficacy population consisted of 100 participants (placebo, n=34; Ostarine 1 mg, n=32; Ostarine 3 mg, n=34). Compared to baseline, in both Ostarine groups (Ostarine 1 mg median 1 5 kg, range −2 1 to 12 6, p=0 0012; Ostarine 3 mg 1 0 kg, -4 8 to 11 5, p=0·046). The change in total lean body mass (median 0·02 kg, range –5·8-6·7) within the placebo group was not significant (p=0·88). The most common serious adverse events were progression of malignant neoplasm (8/ 52 [15%] placebo vs 53 five [9%] Ostarine 1 mg vs seven 54 [13%] Ostarine 3 mg), pneumonia (two [4%] vs two [4%] vs three [6%]), and febrile neutropenia (three [6% vs one [2%] vs none). None of these incidents were considered related to drug work. Both 1mg and 3mg of Ostarine resulted in increases in lean body mass in patients with advanced cancer, compared with baseline measurements. No significant change from baseline was noted in patients assigned placebo. Adverse events were generally very similar between groups, and this was consistent for patients receiving chemotherapy.
OSTARINE MAY BE USEFUL IN THE TREATMENT OF DIABETES
In the same clinical study (2007-2008) Ostarine also significantly reduced fasting glucose levels, and a trend towards reduction in blood insulin was observed. These effects resulted in a reduction in insulin resistance from baseline in the 1 mg and 3 mg treatment groups calculated according to HOMA-IR. Note, this type of reduction in insulin resistance was similar to that observed with metformin and glipizide, the drugs used to treat diabetes. Low levels of testosterone in men are associated with insulin resistance and type II diabetes, while testosterone therapy is known to improve metabolic parameters. This observation may have potential implications for the use of Ostarine in prediabetic or diabetic individuals, as is commonly seen in patients with chronic kidney disease, chronic obstructive pulmonary disease, or metabolic syndrome. Compared to placebo, Ostarine also decreased total cholesterol, HDL, and triglycerides.
OSTARINE AND BODYBUILDING
Similar to anabolic steroids, Ostarine can assist in achieving significant muscle gains. However, its safety profile is significantly better compared to steroids. Ostarine has significantly less dangerous and unwanted side effects, and the potential health risks are many times lower than those that steroid use can cause. For this reason, Ostarine is often used (abuse) by bodybuilders, athletes and people who are trying to gain muscle figure, who want to achieve similar results when using anabolic steroids, but also want to eliminate / minimize possible unwanted side effects. Here, consider it necessary to emphasize that ostarine is not an approved dietary supplement or stimulant for athletes. It is an experimental substance currently under investigation, its long-term effects are not yet fully known and more research is needed. Note that Ostarine, like all other products, is sold for scientific and research clinical use only.
OSTARINE AND DOPING
WADA (World Anti-Doping Agency) banned all Selective androgen receptor modulators (including Ostarin) as early as 2008. Ostarine falls into the S1 Anabolic Agent category of WADA “Prohibited List” prohibited substances. There are many known cases of sports doping with Ostarine among professional athletes, and the number of positive tests on Ostarine has increased in recent years.
POSSIBLE BENEFITS SCIENTIFICALLY INVESTIGATED
Significant and selective anabolic effect on muscles and bones, without strong androgenic side effects on other organs
May help treat serious diseases associated with muscle wasting
May help treat osteoporosis
May be useful in the treatment of diabetes
Helps build and maintain muscle mass
Increases bone mineral density
Lowers glucose levels and improves insulin sensitivity
Helps reduce excess fat
ADVANTAGES OF OSTARINE ON ANABOLIC-ANDROGENIC STEROIDS
Ostarine (MK-2866) is selective and primarily intended for movement in muscles and bones. Due to this selectivity, it does not cause strong androgenic negative effects on other organs, unlike anabolic steroids.
Similar to anabolic steroids, Ostarine can help you achieve significant muscle gains, but has significantly less dangerous and unwanted side effects, and the potential health risks that steroid use can cause are many times lower than that:
Ostarine does not convert to Estrogens or Dihydrotestosterone
Ostarine does not cause gynecomastia
Ostarine does not cause significant retention of water and salts
Ostarine does not cause increased cortisol and estrogen levels
Ostarine Does not have a heavy load for the liver
Ostarine does not cause prostate enlargement.
Ostarine does not cause kidney disease
Ostarine does not cause acne and oily skin
Ostarine does not cause hair loss and baldness
Ostarine does not cause swollen face
Ostarine does not cause excessive facial or body hair (hirsutism).
Ostarine does not cause mood swings
Ostarine does not cause nervousness, irritability, depression, restlessness
Ostarine does not cause aggression, explosiveness and psychological problems.
Ostarine is extremely effective when administered orally (no injections needed)
OSTARINE (MK-2866) FAQ
What is Ostarine MK-2866?
SARM Ostarine (MK-2866) is an oral, nonsteroidal and selective androgen receptor modulator, developed for the treatment of conditions such as muscle wasting and osteoporosis.
What does Ostarine do?
Ostarine has been shown to increase lean body mass, decrease fat mass, and improve modest homeostatic model evaluation (HOMA), a measure of insulin sensitivity.
What is Ostarine used for?
Ostarine can help treat serious diseases associated with muscle wasting and osteoporosis. But it is currently still under investigation.
Does Ostarine build muscle?
Results of clinical studies have confirmed that Ostarine can aid in increasing muscle mass, has strong anabolic properties, and moreover, it only acts selectively in tissues where it is required, in muscles and bones.
Does Ostarine have any strong side effects?
In clinical studies, Ostarine appeared to be safe and well tolerated. It is highly selective and binds to androgen receptors in the body only where it is desired, in muscles and bones. Because of this selectivity, it is also many times less likely to have mild, fewer, and less dangerous side effects than steroids.
Does Ostarine cause gynecomastia?
Ostarine does not cause gynecomastia, because it does not interact with aromatase enzymes.
Is Ostarine dangerous for the prostate?
Ostarine is selective for its muscle and bone only action, it does not convert to dihydrotestosterone, therefore, unlike anabolic steroids, it does not pose a risk to the prostate.
Does Ostarine cause increased cortisol production?
Ostarincortisol does not affect levels and does not increase its production in the body.
Is ostarine banned in sports?
Yes, Ostarine falls into the S1 Anabolic Agent category of WADA “Prohibited List” prohibited substances.
Is Ostarine low testosterone?
Ostarine may suppress production and reduce natural Testosterone levels, but some anabolic steroids much less. The effect on reducing testosterone production is also affected by the size of the dose and the length of use.
How safe is Ostarine?
In clinical studies, Ostarine showed a dose-dependent improvement in total lean body mass and physical function and was generally well tolerated. It is the best and best SARM clinically tested to date.
Does Ostarine increase DHT?
Ostarine does not convert to estrogen and DHT. Since it does not have a steroid structure, reductase and aromatase enzymes (responsible for the conversion of androgens to DHT and estrogens) are not able to participate.
OSTARINE DOSAGE
A common dose in clinical studies that showed a significant increase in lean body mass was 3 mg of Ostarine daily. Among bodybuilders and users who have used Ostarine to build muscle and gain muscle figure, several times higher doses, in the range of 10-30 mg of Ostarine per day, are most often mentioned, in various online forums and Internet discussions. Due to the long half-life of Ostarine, one dose is sufficient for one day.
We emphasize that Ostarine is not an approved dietary supplement or stimulant for athletes. It is an experimental substance still under investigation and not all of its side effects are known. Note that Ostarine, like all other products, is sold for scientific and research clinical use only.
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