产品说明
应用
GW9508, a selective FFA1/GPR40 agonist, may be used to differentiate and characterize the free fatty acid receptor FFA1/GPR40. GW9508 is used to study the role of FFA1/GPR40 receptors in processes such as the free fatty acid enhancement of glucose-stimulated insulin release and type 2 diabetes. GW9508 is used to study the process by which FFA1/GPR40 receptors protect from ovariectomy-induced bone loss in vivo though inhibition of osteoclast differentiation and suppress complete Freund′s adjuvant (CFA)-Induced inflammatory chronic pain.
GW9508 has been used in:
包装
5, 25 mg in glass bottle
生化/生理作用
GW9508 is a selective FFA1/GPR40 agonist. GPR40 was formerly an orphan G protein-coupled receptor whose endogenous ligands have now been identified as free fatty acids (FFAs). The receptor, named FFA receptor 1, has been implicated in the pathophysiology of type 2 diabetes and is a drug target because of its role in FFA-mediated enhancement of glucose-stimulated insulin release. GW9508 showed greater than 500-fold selectivity for GPR40 over GPR41 and GPR43 and possessed a good in vitro and in vivo profile with excellent bioavailability. GW9508 stimulated intracellular Ca2+ mobilization in human embryonic kidney HEK-293 cells expressing GPR40 or GPR120, but not in the parent HEK-293 cell line. GW9508 dose dependently potentiated glucose-stimulated insulin secretion in MIN6 cells, but not in primary rat or mouse islets. GW9508 potentiates the KCl-mediated increase in insulin secretion in MIN6 cells.
基本信息
经验(实验)分子式 | C22H21NO3 |
分子量 | 347.41 |
MDL编号 | MFCD09753282 |
PubChem化学物质编号 | 329799992 |
NACRES | NA.25 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white |
溶解性 | DMSO: >20 mg/mL |
储存温度 | 2-8℃ |
SMILES string | OC(=O)CCc1ccc(NCc2cccc(Oc3ccccc3)c2)cc1 |
InChI | 1S/C22H21NO3/c24-22(25)14-11-17-9-12-19(13-10-17)23-16-18-5-4-8-21(15-18)26-20-6-2-1-3-7-20/h1-10,12-13,15,23H,11,14,16H2,(H,24,25) |
InChI key | DGENZVKCTGIDRZ-UHFFFAOYSA-N |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
个人防护装备 | dust mask type N95 (US), Eyeshields, Faceshields, Gloves |
Sigma-Aldrich