G9797
GW9508
≥98% (HPLC)
Synonym(s):
4-(3-Phenoxybenzylamino)phenylpropionic acid
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About This Item
Empirical Formula (Hill Notation):
C22H21NO3
CAS Number:
Molecular Weight:
347.41
MDL number:
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.25
Assay
≥98% (HPLC)
form
powder
color
white
solubility
DMSO: >20 mg/mL
storage temp.
2-8°C
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
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. 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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
Certificates of Analysis (COA)
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Claire Philippe et al.
Experimental cell research, 319(19), 3035-3041 (2013-08-27)
GW9508 is a free fatty acid receptor agonist able to protect from ovariectomy-induced bone loss in vivo thought inhibition of osteoclast differentiation in a G-coupled Protein Receptor 40 (GPR40)-dependent way. In this study, we questioned whether higher doses of GW9508
Different effects of GPR120 and GPR40 on cellular functions stimulated by 12-O-tetradecanoylphorbol-13-acetate in melanoma cells
Fukushima K, et al.
Biochemical and Biophysical Research Communications, 475(1), 25-30 (2016)
Different roles of GPR120 and GPR40 in the acquisition of malignant properties in pancreatic cancer cells
Fukushima K, et al.
Biochemical and Biophysical Research Communications, 465(3), 512-515 (2015)
Jiayi Huang et al.
Journal of natural products, 82(2), 194-204 (2019-02-14)
Astragalus membranaceus root, Huang Qi in Chinese, is a popular medicinal herb traditionally used to regulate blood glucose. Herein, the identification and characterization of two families of cysteine-rich peptides (CRPs), designated α- and β-astratides, from A. membranaceus roots are reported.
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
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