GW501516

GW501516 C화학적 특성, 용도, 생산

생물학적 활성

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

GW501516 준비 용품 및 원자재

원자재

준비 용품

GW501516 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hubei Langyou International Trading Co., Ltd	+8618874586545	linda@xrdchem.cn	China	197	58
Wuhan Aoliqisi New Material Technology Co., Ltd.	+86-13545906766; +8613545906766	sales@whaop.com	China	265	58
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12456	58
Nantong Guangyuan Chemicl Co,Ltd	+undefined17712220823	admin@guyunchem.com	China	616	58
Guangdong Tuoyuan Biotechnology Co., LTD	+85267545345	sterodschina@gmail.com	China	129	58
WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD	+8615377521700	wangwendy93@gmail.com	China	868	58
Hebei Qige Biological Technology Co. Ltd	+86 +8618733132031		CHINA	1313	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	29220	58
Wuhan Golt Biotech Co., Ltd.	+8615389281203	maria@goltbiotech.com	China	980	58
Shanghai Qianyi New Material Co., Ltd.	+8618083322317	3391883138@qq.com	China	878	58