371830
GPR40 Antagonist, GW1100
The GPR40 Antagonist, GW1100, also referenced under CAS 306974-70-9, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.
别名:
GPR40 Antagonist, GW1100, 1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone, SB376752
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所有图片(2)
About This Item
推荐产品
质量水平
方案
≥97% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 50 mg/mL
运输
wet ice
储存温度
2-8°C
SMILES字符串
FC(C=C1)=CC=C1CSC(N(C2=CC=C(C(OCC)=O)C=C2)C=C3CC4=CN=C(N=C4)OCC)=NC3=O
InChI
1S/C27H25FN4O4S/c1-3-35-25(34)20-7-11-23(12-8-20)32-16-21(13-19-14-29-26(30-15-19)36-4-2)24(33)31-27(32)37-17-18-5-9-22(28)10-6-18/h5-12,14-16H,3-4,13,17H2,1-2H3
InChI key
PTPNCCWOTBBVJR-UHFFFAOYSA-N
一般描述
A cell-permeable pyrimidinylmethyl-pyrimidinone compound that acts as potent, reversible and non-competitive GPR40 antagonist. Selectively blocks GPR40-mediated intracellular Ca2+ release stimulated by GPR40 Agonist GW9508 (Cat. No. 371706) and linoleic acid (pIC50 of 5.99 in GPR40 expressing HEK293 cells) with no effect on GPR120-mediated activation. Shown to significantly reverse glucose-induced insulin secretion potentiated by GW9508 and only partially reduce linoleic acid effect in MIN6 cells.
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Stoddart, L.A., et al. 2007. Mol. Pharmacol.71, 994.
Briscoe, C.P., et al. 2006. Br. J. Pharmacol.148, 619.
Briscoe, C.P., et al. 2006. Br. J. Pharmacol.148, 619.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Katarzyna Bazydlo-Guzenda et al.
Molecular pharmacology, 100(4), 335-347 (2021-08-06)
G protein-coupled receptor (GPR) 40 is a free fatty acid receptor mainly expressed in pancreatic β-cells activated by medium- and long-chain fatty acids and regulating insulin secretion via an increase in cytosolic free calcium ([Ca2+]i). Activation of GPR40 in pancreatic
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