SARMS
  • GW-501516 (Cardarine) - 20mgs/ml @ 30ml
    GW-501516 (Cardarine) - 20mgs/ml @ 30ml

    GW-501516 (Cardarine) - 20mgs/ml @ 30ml

    Brand: SARMS1 Model:GW-501516 Availability: In Stock
    Price: $99.99 $149.99
    Based on 1 reviews.

    GW-501516 - 30ml @ 20mgs/ml

    ***SHAKE WELL BEFORE RESEARCH***

     

    {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]-2-methylphenoxy}acetic acid

    GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARd modulator. GW 501516 activates AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue, and GW 501516 has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome, most likely by stimulating fatty acid oxidation. It has been proposed as a potential treatment for obesity and related conditions, especially when used in conjunction with a synergistic compound AICAR, as the combination has been shown to significantly increase exercise endurance in animal studies.

    GW-50156 regulates fat burning through a number of widespread mechanisms; it increases glucose uptake in skeletal muscle tissue and increases muscle gene expression, especially genes involved in preferential lipid utilization. This shift changes the body’s metabolism to favor burning fat for energy instead of carbohydrates or muscle protein, potentially allowing clinical application for obese patients to lose fat effectively without experiencing muscle catabolism or the effects and satiety issues associated with low blood sugar. GW-501516 also increases muscle mass, which improved glucose tolerance and reduced fat mass accumulation even in mice fed a very high fat diet, suggesting that GW-501516 may have a protective effect against obesity.
     

    GW501516 is a selective agonist  (activator) of the PPARδ receptor.  It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ with > 1000 fold selectivity over PPARα and PPARγ.

    In rats, binding of GW501516 to PPARδ recruits the co activator PGC-1a. The PPARδ/coactivator complex in turn up regulates the expression of proteins involved in energy expenditure.  Furthermore in rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed. In obese rhesus monkeys, GW501516 increased high-density lipoprotein  (HDL) and lowered very-low-density lipoprotein (VLDL).  The mechanism by which PPARδ agonists increase HDL appears to be a result of increased expression of the cholesterol transporter ABCA1.
     

    This article is intended for educational / informational purposes only. THIS PRODUCT IS INTENDED AS A RESEARCH CHEMICAL ONLY. This designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. Bodily introduction of any kind into humans or animals is strictly forbidden by law.

  • LGD-4033 - 10mgs/ml @ 30ml
    LGD-4033 - 10mgs/ml @ 30ml

    LGD-4033 - 10mgs/ml @ 30ml

    Brand: SARMS1 Model:LGD-4033 Availability: In Stock
    Price: $99.99 $249.99
    Based on 1 reviews.

    LGD-4033 - 30ml @ 10mgs/ml

    ***SHAKE WELL BEFORE RESEARCH***

    LGD-4033 is a selective androgen receptor modulator a novel non-steroidal, oral SARM that binds to AR with high affinity (Ki of ~1 nM) and selectivity, class of androgen receptor (AR) ligands that is tissue selective, developed to treat muscle wasting associated with cancer, acute and chronic illness and age-related muscle loss. LGD-4033 is expected to produce the therapeutic benefits of testosterone with improved safety, tolerability and patient acceptance due to tissue-selective mechanism of action and an oral route of administration. It demonstrates anabolic activity in muscles, anti-resorptive and anabolic activity in bones and a robust selectivity for muscle and bone versus prostate and sebaceous glands. LGD-4033 has recently completed a Phase I Multiple Ascending Dose study in healthy volunteers this randomized, double-blind, placebo-controlled Phase I study established the safety and tolerability up to doses of 22 mg.

     

    Clinical Experience

    Phase I single and multiple dose escalation studies of LGD-4033 were conducted in a total of 116 healthy male subjects. The safety, tolerability and preliminary efficacy of LGD-4033 was evaluated in the double-blind, placebo-controlled Phase I multiple ascending dose study. Healthy male subjects were randomized to receive 0.1, 0.3 or 1.0 mg LGD-4033 or placebo once daily over 21 days.

    Key findings of this study include:

     LGD-4033 was safe and well tolerated at all doses following daily oral administration for three weeks in young healthy males 

     No clinically significant dose-related adverse events were reported 

     No clinically significant changes in liver function tests, PSA, hematocrit or ECG were seen 

     Positive dose-dependent trends in lean muscle mass increase were observed with drug-treated subjects 

     Positive dose-dependent trends in functional exercise and strength measures were consistent with anabolic activity

    LGD-4033 is positioned to enter into Phase II development. Studies are planned to evaluate LGD-4033 over 12-weeks of oral dosing in conditions such as muscle wasting associated with cancer, acute rehabilitation (e.g. hip fracture), and acute illness.

    Cachexia is a wasting syndrome defined by progressive weight loss, anorexia, and muscle atrophy. Cachexia is a significant factor in the poor performance status and high mortality rate of patients in multiple disease states such as cancer, COPD, severe burns, AIDS and end stage renal disease. Cachexia significantly impairs quality of life and response to medical treatment. Approximately 25% of all cancer deaths can be attributed to cachexia.
     

    LGD-4033 has the potential to prevent and treat a variety of muscle wasting conditions:

    *This article is intended for educational / informational purposes only. THIS PRODUCT IS INTENDED AS A RESEARCH CHEMICAL ONLY. This designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. Bodily introduction of any kind into humans or animals is strictly forbidden by law.

  • MK-2866 (Ostarine) - 50mg/ml @ 30ml
    MK-2866 (Ostarine) - 50mg/ml @ 30ml

    MK-2866 (Ostarine) - 50mg/ml @ 30ml

    Brand: SARMS1 Model:mk-2866 Availability: In Stock
    Price: $99.99 $299.99
    Based on 1 reviews.

    Mk-2866 (Ostarine) - 30mls @ 50mgs/ml

    ***SHAKE WELL BEFORE RESEARCHING***

     

    Mk-2866 (Ostarine) - 30mls @ 50mgs/ml

    ***SHAKE WELL BEFORE RESEARCHING***

     

    ((2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide)

     

    Ostarine (MK-2866) also known as “Enobosarm” is an investigational selective androgen receptor modulator (SARM) from GTX.Inc. for treatment of conditions such as mucsle wasting and osteoporosis, formerly under development by Merck & Company.

     

    Ostarine exerts its anabolic effects on skeletal muscle tissue almost exclusively, and therefore represents a new potential treatment option for a wide spectrum of conditions from age-related muscular atrophy (sarcopenia), AIDS or cancer-related wasting/cachexia, and even an agent to minimize atrophy during recovery periods from serious surgery or similar situations. It is effective in not only maintaining lean body mass (LBM) but actually increases it:

    In the study, Ostarine met the primary endpoint of LBM, measured by a dual energy X-ray absorptiometry (DEXA) scan, by demonstrating statistically significant increases in LBM compared to baseline in both the Ostarine 1 mg and 3 mg treatment cohorts. Specifically, the change from baseline in LBM for the placebo, 1 mg and 3 mg treatment groups was 0.1 kg (p=0.874 compared to baseline), 1.5 kg (p=0.001) and 1.3 kg (p=0.045), respectively, at the end of the 16-week trial.

     

    Dr. Adrian Dobs, MD, MHS, an investigator in the Phase II trial for treatment of cancer cachexia, had the following to say about MK-2688:

    Approximately half of all cancer patients suffer from the devastating effects of cancer induced muscle loss. Increasing lean body mass may improve patients' quality of life and even their response to cancer treatment. These Phase II results demonstrate the potential of a SARM to fill an important unmet need as there are currently no FDA-approved therapies available for cancer cachexia.

     

    As mentioned above as well as by Dobs, there exist few treatments for cachexia, no FDA-approved indicated treatments, and certainly no ideal treatments; the same is true of the majority of muscle-wasting conditions.  Muscle-wasting related to cancer is the cause of a full 20% of cancer-related deaths, and it is likely that in related and similar conditions the instance of morbidity is equally high.

     

    As mentioned by Furuya, the effects of MK-2688 translate to anabolism in bone as well as skeletal muscle tissue, which means it could be indicated in an extremely wide variety of uses such as osteoporosis and as a concurrent treatment with drugs that reduce bone density, such as the class of cancer-treatment drugs known as selective estrogen receptor modulators:

    Many efforts to produce novel drug materials maintaining a desired biological activity with an adequate tissue selectivity, which is so-called selective androgen receptor modulators (SARMs) , are being performed. As one of such efforts, studies on SARMs against bone tissues which possess a significant potential to stimulate a bone formation with reducing undesirable androgenic virilizing activities are in progress all over the world.

     

    *This article is intended for educational / informational purposes only. THIS PRODUCT IS INTENDED AS A RESEARCH CHEMICAL ONLY. This designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. Bodily introduction of any kind into humans or animals is strictly forbidden by law.

  • S4 (Andarine) - 50mgs/ml @ 30ml
    S4 (Andarine) - 50mgs/ml @ 30ml

    S4 (Andarine) - 50mgs/ml @ 30ml

    Brand: SARMS1 Model:S4 (Andarine) Availability: In Stock
    Price: $79.99 $149.99
    Based on 1 reviews.

    S4 (Andarine) - 30ml @ 50mgs/ml

    ***SHAKE WELL BEFORE RESEARCH***

     

    (2S)-3-(4-acetamido-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide

    S4 (Andarine) is an investigational selective androgen receptor modulator (SARM) developed by GTX.INC for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy, us the non-steroidal androgen antagonist bicalutamide as a lead compound.

    Andarine is an orally active partial agonist for androgen receptors. In an animal model of benign prostatic hypertrophy, andarine was shown to reduce prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or anti-androgenic side effects.This suggests that it is able to competitively block binding of dihydrostestosterone to its receptor targets in the prostate gland, but its partial agonist effects at androgen receptors prevent the side effects associated with the anti-androgenic drugs traditionally used for treatment of BPH.

    S-4 (3 mg/kg/day) was also able to restore skeletal muscle (i.e., soleus muscle) and strength in castrated rats, important and applicable for the treatment of muscle wasting and male HRT.

    A 120-day study comparing SARM S-4 and dihydrotestosterone (DHT) treatment in ovariectomized rats demonstrated that S-4 was able to maintain bone mass and bone strength to the levels of intact controls and exhibited greater efficacy than DHT.

    Testosterone shows a very similar increase in muscle and prostate growth in a dose dependent manner where S-4 shows a great increase in muscle growth with prostate growth staying largely uniform.

    S-4 also demonstrated the ability to improve skeletal muscle strength, increase lean body mass (LBM), reduce body fat, and prevent bone loss.


     

    This article is intended for educational / informational purposes only. THIS PRODUCT IS INTENDED AS A RESEARCH CHEMICAL ONLY. This designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. Bodily introduction of any kind into humans or animals is strictly forbidden by law.

     

     

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