GW-501516

GW 501516 (or Cardarine) is a research chemical developed in the 90s of the 20th century to prevent and treat tumor formation in the colon, prostate and breast. Studies conducted in the early 21st century have found that GW 501516 and other PPAR agonists are also able to block metabolic disorders such as obesity and diabetes through specific gene expression.

$70.00

Purity:

99.9%

Form:

Powder

Packaging:

Hidden Packaging

Transportation:

Door to door

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SPECIFICATION

GW501516 Basic information

Product Name:	GW501516
Synonyms:	GW501516;2-METHYL-4-((4-METHYL-2-(4-TRIFLUOROMETHYLPHENYL)-1,3-THIAZOL-5-YL)-METHYLSULFANYL)PHENOXY-ACETIC ACID
CAS:
MF:	C21H20F3NO3S2
MW:	455.51
EINECS:
Product Categories:
Mol File:	Mol File

GW501516 Chemical Properties

Melting point	134 - 144°C
storage temp.	Refrigerator
solubility	DMSO (Slightly), Methanol (Slightly)
form	Solid
color	White to Pale Yellow

GW501516 Usage And Synthesis

Uses	An experimental drug meant to control lipids and increase the level of HDL, or good cholesterol, in the bloodstream.A cell-permeable, thiazolyl compound that acts as a potent, high affinity, PPARδ agonist. Exhibits selectivity for PPARδ compared to PPARα and PPARγ. Does not exibit any activity against other nuclear or non-nuclear receptors. Reported to increase cholesterol efflux and ABAC1 expression in macrophages, fibroblasts, and intestinal cells. GW 501516 has been found to enhance endurance in mice without any training.
Biological Activity	GW 501516 is shown to be the most potent and selective PPARα agonists known with an EC50 of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ. 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.
Synthesis	Add Cs2CO3 (3.25 g, 10.0 mmol), followed by the chloromethylthiazole (2.60 g) to a stirred solution of 4-mercapto-2-methylphenol (1.40 g) in CH3CN (80 mL). Stir the reaction mixture at room temperature for 4 hours. Add Cs2CO3 (4.89 g, 15.0 mmol), followed by methyl bromoacetate (1.23 mL, 13.0 mmol) to the mixture. Stir the reaction mixture at room temperature for another 5 hours. Pour the mixture into water. Extract the mixture with EtOAc (3 x 100 mL). Combine the organic layers. Wash the organic layers with brine. Dry the organic layers (Na2SO4). Concentrate the organic layers. Purify the residue by column chromatography on silica gel with hexane/ ethyl acetate (5:1). 1H NMR (CDCl3) δ7.97 (d, 2H, J= 8.4 Hz), 7.65 (d, 2H, J= 8.4 Hz), 7.21 (d, 1H, J= 2.4 Hz), 7.13 (dd, 1H, J= 8.4, 2.4 Hz), 6.58 (d, 1H, J= 8.4 Hz), 4.63 (s, 2H), 4.11 (s, 2H), 3.78 (s, 3H), 2.24 (s, 3H), 2.20 (s, 3H). 13C NMR (CDCl3) δ169.2, 163.0, 156.3, 151.3, 136.8, 136.1, 132.1, 131.2 (q, J= 32 Hz), 130.6, 128.4, 126.3, 125.8 (q, J= 4 Hz), 125.3, 122.1, 111.4, 65.4, 52.2, 32.4, 16.1, 14.8. 19F NMR (CDCl3) δ115.5 (s). Fig. The synthetic step 1 of GW-501516