G9797
GW9508
≥98% (HPLC)
别名:
4-(3-Phenoxybenzylamino)phenylpropionic acid
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经验公式（希尔记法）:
C22H21NO3
化学文摘社编号:
分子量:
347.41
NACRES:
NA.25
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
InChI key
DGENZVKCTGIDRZ-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
powder
color
white
solubility
DMSO: >20 mg/mL
storage temp.
2-8°C
Quality Level
Application
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.
Biochem/physiol Actions
GW9508 is a selective FFA1/GPR40 agonist.
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
法规信息
新产品
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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
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
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
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
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