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Merck
CN

G9797

Sigma-Aldrich

GW9508

≥98% (HPLC)

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别名:
4-(3-Phenoxybenzylamino)phenylpropionic acid
经验公式(希尔记法):
C22H21NO3
分子量:
347.41
MDL编号:
UNSPSC代码:
51111800
PubChem化学物质编号:
NACRES:
NA.25

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white

溶解性

DMSO: >20 mg/mL

储存温度

2-8°C

SMILES字符串

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

应用

GW9508 has been used in:
  • cell proliferation assay in pancreatic cancer cells
  • in motility assay in melanoma cells
  • cell invasion assay in colon cancer cells

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.

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.

WGK

WGK 3

个人防护装备

dust mask type N95 (US), Eyeshields, Faceshields, Gloves

法规信息

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Habtamu Wondifraw Baynes et al.
Adipocyte, 7(2), 81-87 (2018-03-15)
Polyunsaturated Fatty acids have multiple effects in peripheral tissues and pancreatic beta cell function. The n-3 Polyunsaturated Fatty acids prevent and reverse high-fat-diet induced adipose tissue inflammation and insulin resistance. Insulin secretion is stimulated by glucose, amino acids, and glucagon-
Chiori Yabuki et al.
PloS one, 8(10), e76280-e76280 (2013-10-17)
Selective free fatty acid receptor 1 (FFAR1)/GPR40 agonist fasiglifam (TAK-875), an antidiabetic drug under phase 3 development, potentiates insulin secretion in a glucose-dependent manner by activating FFAR1 expressed in pancreatic β cells. Although fasiglifam significantly improved glycemic control in type
Maria Fernanda Graciano et al.
Islets, 5(4), 139-148 (2013-07-03)
G protein coupled receptor 40 (GPR40) and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase complex have been shown to be involved in the fatty acid amplification of glucose-stimulated insulin secretion (GSIS). The effect of palmitic acid on superoxide production and insulin
Jie Xiao et al.
Journal of neuroinflammation, 18(1), 160-160 (2021-07-20)
Germinal matrix hemorrhage (GMH) is defined by the rupture of immature blood vessels in the germinal matrix, where subsequent hemorrhage enters the subependymal zone and the cerebral lateral ventricles. The consequent blood clot has been identified as the causative factor
Yufeng Zhao et al.
PloS one, 8(4), e60255-e60255 (2013-04-09)
The role of the free fatty acid (FFA) receptor and the intracellular metabolites of linoleic acid (LA) in LA-stimulated increase in cytosolic free calcium concentration ([Ca(2+)]i) was investigated. [Ca(2+)]i was measured using Fura-2 as indicator in rat pancreatic β-cells in

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