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GW 501516

Catalog No. T6151 CAS 317318-70-0

Synonyms: Cardarine, GW501516, GW 1516, GSK-516, Endurobol

GW 501516 (Endurobol) is a effective and highly specifc PPARβ/δ agonist (EC50: 1 nM), with 1000-fold selectivity over hPPARα/γ.

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GW 501516, CAS 317318-70-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 66.00
25 mg	In stock	$ 113.00
50 mg	In stock	$ 153.00
100 mg	In stock	$ 215.00
200 mg	In stock	$ 348.00
500 mg	In stock	$ 532.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.94%

Purity: 98.91%

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Description	GW 501516 (Endurobol) is a effective and highly specifc PPARβ/δ agonist (EC50: 1 nM), with 1000-fold selectivity over hPPARα/γ.
Targets&IC50	PPARδ:1 nM(Ki)
In vitro	GW 501516 is shown to be the most potent and selective PPARδ agonist as known with an EC50 of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ[1]. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner[3].
In vivo	GW 501516 adversely affects bone formation, resulting in reduced bone mineral density (BMD) and compromised bone integrity in ovariectomized (OVX) rats[2]. Additionally, it mitigates interstitial inflammation and damage to proximal tubular cells in a mouse model of protein-overload nephropathy[3]. Furthermore, treatment with GW 501516 improves running endurance and increases the number of succinate dehydrogenase (SDH)-positive muscle fibers in both conditioned and unconditioned mice[4].
Kinase Assay	Tyrosine Kinase Assays: Enzyme assays for determination of IC50 are performed in 96-well filter plates in a total volume of 0.1 mL, containing 20 mM Hepes, pH 7.4, 50 mM sodium vanadate, 40 mM magnesium chloride, 10 μM adenosine triphosphate (ATP) containing 0.5 mCi of [32P]ATP, 20 mg of polyglutamic acid/tyrosine, 10 ng of EGFR tyrosine kinase, and appropriate dilutions of CI-1033. All components except the ATP are added to the well and the plate is incubated with shaking for 10 min at 25 °C. The reaction is started by adding [32P]ATP, and the plate is incubated at 25 °C for another 10 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid (TCA). The plate is kept at 4 °C for at least 15 min to allow the substrate to precipitate. The wells are then washed five times with 0.2 mL of 10% TCA and 32P incorporation determined with a Wallac β plate counter.
Cell Research	GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 μM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 μM palmitate bound to 8.0% BSA for 12 h[3].

Synonyms	Cardarine, GW501516, GW 1516, GSK-516, Endurobol
Molecular Weight	453.5
Formula	C21H18F3NO3S2
CAS No.	317318-70-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.4 mg/mL(100 mM)

References and Literature

1. Wei ZL, et al. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8. 2. Chen, W., Gao, R., Xie, X., Zheng, Z., Li, H., & Li, S. et al. (2015). A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice. Scientific Reports, 5(1). doi: 10.1038/srep09884

Citations

1. Han W, Wang N, Kong R, et al. Ligand-activated PPARδ expression promotes hepatocellular carcinoma progression by regulating the PI3K-AKT signaling pathway. Journal of Translational Medicine. 2022, 20(1): 1-14. 2. Ren Q, Xie X, Zhao C, et al. 2, 2′, 4, 4′-Tetrabromodiphenyl Ether (PBDE 47) Selectively Stimulates Proatherogenic PPARγ Signatures in Human THP-1 Macrophages to Contribute to Foam Cell Formation. Chemical Research in Toxicology. 2022

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Lipid Metabolism Compound Library Anti-Obesity Compound Library Human Metabolite Library Anti-Hypertension Compound Library Bioactive Compounds Library Max NO PAINS Compound Library

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Keywords

GW 501516 317318-70-0 Autophagy DNA Damage/DNA Repair Metabolism PPAR GW-501516 Inhibitor Peroxisome proliferator-activated receptors GSK 516 Cardarine GW1516 GW501516 inhibit GW 1516 GSK-516 Endurobol GSK516 GW-1516 inhibitor

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