Archive for Selective estrogen receptor modulator

GW-501516 – THE ULTIMATE PERFORMANCE ENHANCER

GW-501516 is a drug that acts as a PPARδ modulator. GW-501516 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. GW-501516 activates the AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue.

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.

GW-501516 has also shown to dramatically increase endurance and recovery. 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.

In obese rhesus monkeys, GW-501516 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.

GW-501516 Beneficial Uses:

GW-501516 has many benefits but has two primary uses. The most common use of GW consists of the extreme amount of endurance and recovery increase. The results with GW-501516 use regarding endurance increase are staggering. GW was banned by the WADA (World Anti Doping Association) in 2009 because it provided such a large advantage to users over their competition. GW has shown to be fast acting with drastic results. A user can expect to see an endurance increase within a few days of use. GW-501516 provides continuous increases in the VO2MAX, allowing an individual to provide maximal output during exercise, thus obtaining the name, “The Ultimate Performance Enhancer.” The common dosage for this type of result is 20 mg a day with 14 weeks of continuous use

The other main use of GW-501516 is to aid in fat loss. GW-501516 has shown to melt away fat at a rapid pace. Another strong component of GW-501516 is that it is non catabolic, meaning it allows a user to lose fat and not have to sacrifice muscle. Many people that are on a fat burning diet are sacrificing a lot of muscle. GW-501516 allows a user to hold on to much more muscle than a standard fat lass diet or other fat loss compound would allow. GW-501516 also shines when ran in conjunction with other SARMS. When stacking GW-501516 with Ostarine and S4, users can add lean muscle while still losing weight and body fat. This makes GW-501516 highly desirable for many. The most optimal dosage for fat loss is 20 mg a day but users will still be able to receive this benefit at 10 mg a day.

GW 501516 can be ran in 8-12 cycles and can also be ran in conjunction with any SARM, steroid or supplement. As with any other steroid or supplement, it should be cycled properly to avoid any possible side effects and the keep it as effective as possible.

GW-501516 Dosing Timing:

GW-501516 also has a very long half life, so it can be dosed once a day or split 12 hours apart. The most effective method of dosing is to take it in one serving, 30 minutes prior to working out. On non workout days, once a day dosing in the morning is the best method. If a split dosage is used, 10-12 hour splits are optimal.

GW-501516 Side effects:

There are constant debates and many studies arguing the potential side effects for a user. There are studies showing that GW-501516 has caused cancer in rats while other studies refute it. The ONE study that was conducted that showed this issue was deeply flawed and refuted time and time again. GW-501516 dosing was not only abused but ran at insurmountable amounts of time within this study. When ran properly, it has actually been used as a cancer treatment. There are no known side effects associated with GW use and the only need to cycle off is so that one’s body does not acclimate or desensitize to use. There is no suppression, no toxicity and no other common side effects. This makes GW even more desirable amongst the bodybuilding community.

Benefits of GW-501516:

Extreme increases in endurance and recovery
Extreme fat melting
Long Half Life Making Dosing Optimal
Lowering of Bad Cholesterol and Increasing Good Cholesterol
Minimal Side Effects
Can be ran up to 12 weeks
Stacks well with everything
Non catabolic
Excellent energy
Excellent overall sense of well-being and feeling

 

The Science of GW-501516 Fat Burning

GW-50156 regulates fat burning through a number of widespread mechanisms. GW-501516 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.


 GW-501516 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, GW-501516 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.

Cholesterol Improvement

An often overlooked benefit of GW-501516 use is the ability to treat poor cholesterol. GW was originally formulated to treat people suffering from cholesterol problems and has shown to significantly increase HDL (good cholesterol) while reducing LDL (bad cholesterol).

 

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Raloxifen

Raloxifen

Raloxifen belongs to the class of compounds known as SERMs or selective estrogen receptor modulators. SERMs decrease activity of estrogen and are therefore considered an “anti-estrogen” treatment. However, SERMs do not act by decreasing serum estrogen or aromatase-mediated conversion, but rather through a blocking activity at the estrogen receptor on a cellular level. In other words, raloxifen and its metabolites are active at the estrogen receptor but not as an estrogen-like stimulus (agonist). Instead, they prevent estrogen from exerting its effects at the cellular level. This (as well as other means of blocking estrogenic activity or reducing estrogen levels) creates a rise in testosterone in men because testosterone production is modulated partially via serum estrogen levels.

Raloxifen and its sister drug tamoxifen are typically used in treating estrogen-receptor dependent breast cancer in women[1]. Raloxifen may prove to have more diverse uses than tamoxifen for several reasons:

Selective estrogen receptor modulators (SERMs) or estrogen agonists/antagonists have shown promise in osteoporosis in that they have the potential to reduce the risk of fracture, and also reduce the risk of breast cancer. SERMs maybe classified according to their core structure, which is typically a variation of the 17 beta-estradiol template and sub-classified according to the side chain at the helix 12 affector region. The best known are the triphenylethylenes such as tamoxifen, used in the management of breast cancer. However, the clinical application of this class of SERMs has been limited due to endometrial stimulation. A second class is the benzothiophenes such as raloxifene and arzoxifene, which have skeletal benefit with little, if any, uterine stimulation.[1]

In a study conducted by Christodoulakis et al, “raloxifene users did not exhibit any difference with respect to sex steroids and HOMA-IR levels.”[2]

Raloxifen increased serum testosterone but reduced serum IGF-1 in a study performed by Duschek et al:

In aging men serum levels of testosterone and insulin-like growth factor-1 (IGF-1) decline, potential factors in the reduced muscle strength, abdominal obesity, sexual dysfunction and impaired general well being of aging. The partial estrogen agonist and antagonist raloxifene increase serum testosterone levels in aging men, but the effect of raloxifene on serum IGF-1 levels in men is unknown. In this study the effects of raloxifene on IGF-1 levels and the associated increase in serum testosterone were compared to the effects of oral testosterone supplementation…. RESULTS: Compared to placebo raloxifene increased serum testosterone by 20% but it decreased serum IGF-1 levels by 24.5% (95% confidence interval (CI): -13.0 to -36.1%). No significant change in serum IGFBP-3 levels was found. The effect of raloxifene on serum IGF-1 has been observed with other oral estrogens, and, therefore, is likely to be ascribed to the partial estrogen agonist activity of raloxifene.[3]

According to Nordt et al, raloxifen may hold potential as an intervention in adolescent gynecomastia: “Newer treatment strategies, such as the antiestrogen raloxifene, have shown promising results; however, further studies are needed to determine long-term efficacy. As a result of the limited pharmaceutical treatment options, many more adolescents are seeking surgical intervention.[4]”

As the title of the study suggests, raloxifen is also a promising treatment for male osteoporosis:

Raloxifene has been shown to increase bone mineral density of the hip in men receiving androgen deprivation therapy for prostate cancer. Moreover, experimental data demonstrated dramatic increase in cell death in human prostate cancer cell lines after the treatment with raloxifene. All these observations suggest that SERMs may be useful for the prevention and treatment of osteoporosis not only in postmenopausal women but also in elderly men. However, our hypothesis should be tested in a proper designed clinical trial.[5]

Kastelan goes on to write that there are still issues of dose and duration to be assessed by further clinical study, as well as more markers of health and physical balance to be weighed against the benefits of raloxifen treatment.

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