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Merck
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重要文件

G9797

Sigma-Aldrich

GW9508

≥98% (HPLC)

同義詞:

4-(3-Phenoxybenzylamino)phenylpropionic acid

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About This Item

經驗公式(希爾表示法):
C22H21NO3
CAS號碼:
分子量::
347.41
MDL號碼:
分類程式碼代碼:
51111800
PubChem物質ID:
NACRES:
NA.25
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品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white

溶解度

DMSO: >20 mg/mL

儲存溫度

2-8°C

SMILES 字串

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 密鑰

DGENZVKCTGIDRZ-UHFFFAOYSA-N

應用

GW9508 has been used in:
  • cell proliferation assay in pancreatic cancer cells[1]
  • in motility assay in melanoma cells[2]
  • cell invasion assay in colon cancer cells[3]

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.[4][5]

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

個人防護裝備

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


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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
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
Yuhang Gong et al.
Neuropharmacology, 164, 107899-107899 (2019-12-07)
GPR40 was utilized as the drug target to the treatment of diabetes, but the function and mechanisms ameliorating the Alzheimer's disease (AD) remain unknown. In present study, the typical APP/PS1 mouse model was applied to explore the function and mechanism
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
Yong Yang et al.
Science advances, 4(10), eaau2357-eaau2357 (2018-10-23)
Epilepsy is a common neurological disease, and approximately 30% of patients do not respond adequately to antiepileptic drug treatment. Recent studies suggest that G protein-coupled receptor 40 (GPR40) is expressed in the central nervous system and is involved in the

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