What Is GW 501516 20MG/ML | 60ML?
GW-501516 is also referred to as cardarine or endurobol. It is frequently mistaken for SARM (selective androgen receptor modulator) despite having no effect on androgen receptors. In fact, it belongs to the class peroxisome proliferator-activated receptor agonist. Research shows that it increases fat loss, improves metabolic disorders and boosts strength performance. It has not been approved by the FDA yet. At Pinnacle Peptides, GW-501516 for sale is exclusively available for research and experimentation.
Structure Of GW 501516 20MG/ML | 60ML
From Pubchem
IUPAC Name: 2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid
Synonyms: Endurobol, GW 1516
Molecular Formula: C21H18F3NO3S2
Molecular Weight: 453.5 g/mol
CAS number: 317318-70-0
PubChem CID: 9803963
History
Cardarine was initially developed by the collaboration of two medicinal companies named GSK and Ligand Pharmaceuticals in 1992. Later, GSK sponsored a phase I trial of cardarine for the treatment of hyperlipidemia in 2000, followed by phase I/II in 2002. By 2007, two phase II clinical trials of GW-501516 were completed but GSK abandoned the further development of the drug because of safety reasons.
Mechanism Of GW 501516 20MG/ML | 60ML
Cardarine is an agonist of the peroxisome proliferator-activated receptor delta (PPARδ). It displays high affinity and potency for PPARδ with 1000-fold selectivity over PPARα and PPARγ. PPAR are the receptors found in the nucleus that regulate genes involved in energy metabolism, cell differentiation and various other body processes. Research shows that GW-501516 activates AMP-activated protein kinase, and increases glucose uptake and fatty acid oxidation.
Pre-Clinical/Clinical Research
1. Diabetes
GW-501516 has been shown to improve diabetes and blood glucose levels through activation of AMP-activated protein kinase by PPAR-delta. AMPK is a signal that controls blood glucose levels and gets activated in the presence of low energy levels.
One study was designed to investigate the role of PPARδ agonists in gestational diabetes. Rat models of GDM were tested for fasting blood glucose levels, fasting insulin and insulin sensitivity index on days 3, 7 and 10. After that, their glucose tolerance test was performed on the 20th day of gestation. The findings indicated that treatment with cardarine improved blood glucose tolerance and insulin sensitivity. Furthermore, researchers observed an increased expression of GLUT-2 which is associated with cellular glucose uptake [1].
Furthermore, it has been proposed that peroxisome proliferator-activated receptor agonists might be able to improve diabetic wound healing. One study found that GW-501516 can accelerate wound healing in diabetic rats. Moreover, the researchers suggested that the activation of PPAR-delta stimulated the production of catalase and GPx1 (antioxidant enzymes). These enzymes then reduced the accumulation of H2O2, thus protecting the structure of the extracellular matrix in the wound area [2].
2. Fat loss
Activation of PPARδ has been shown to upregulate the expression of genes involved in beta-oxidation and energy dissipation. One study found that GW-501516 reduced hepatic fat content in overweight patients with mixed hyperlipidemia [3]. Furthermore, it has been shown to increase HDL and decrease triglyceride levels as compared to the placebo. It also increases the expression of CPT1, CD36, and ABCA1, which suggests the increased utilization of peripheral fat [4].
3. Cancer
PPARδ plays an important role in regulating inflammation and cancer. One study conducted on AOM/DDS-induced mice found that the use of GW-501516 was associated with colorectal cancer. The mechanism behind this carcinogenic effect is unclear. However, research shows that it increases the expression of GLUT1 and SLC1A5 in colon cancer cells and enhances the AOM/DDS-induced colorectal tumor. Furthermore, it has also been shown to increase the gene expression of pro-inflammatory cytokines in the inflamed colon [5].
4. Strength Performance
The use of cardarine is popular among the sports community as it is thought to enhance athletic performance. However, to date, there are no human studies available to confirm this effect. Only one study conducted on rats suggests that cardarine can improve strength performance [6].
Summary
GW-501516 is an agonist of the peroxisome proliferator-activated receptor delta that is found in the nucleus. It is involved in the expression of genes responsible for various bodily processes, including energy metabolism. It has been shown to increase fat loss, improve blood glucose control and speed up healing of wounds. Its use is associated with colorectal cancer, and it is not approved by the FDA for therapeutic use. We don’t support its unwarranted use and offer GW-501516 purchase exclusively for research. Only buy GW-501516 if you are a qualified researcher.
References
- Zhou, J., et al., The Role of PPARδ Agosnist GW501516 in Rats with Gestational Diabetes Mellitus. Diabetes, Metabolic Syndrome and Obesity, 2020. 13: p. 2307-2316.
- Wang, X., et al., Early controlled release of peroxisome proliferator-activated receptor β/δ agonist GW501516 improves diabetic wound healing through redox modulation of wound microenvironment. Journal of Controlled Release, 2015. 197: p. 138-147.
- Steensels, S., J. Qiao, and B.A. Ersoy, Transcriptional Regulation in Non-Alcoholic Fatty Liver Disease. Metabolites, 2020. 10(7): p. 283.
- Sprecher, D.L., et al., Triglyceride:high-density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator-activated receptor delta agonist. Arterioscler Thromb Vasc Biol, 2007. 27(2): p. 359-65.
- Zhou, D., et al., PPARδ agonist enhances colitis-associated colorectal cancer. European Journal of Pharmacology, 2019. 842: p. 248-254.
- Chen, W., et al., A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice. Sci Rep, 2015. 5: p. 9884.
Certificate of Analysis (COA)
High Performance Liquid Chromatography (HPLC)
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