G9797

GW9508

≥98% (HPLC)

• Synonym(s): 4-(3-Phenoxybenzylamino)phenylpropionic acid
• Empirical Formula (Hill Notation): C₂₂H₂₁NO₃
• CAS Number: 885101-89-3
• Molecular Weight: 347.41
• MDL number: MFCD09753282
• PubChem Substance ID: 329799992
• NACRES: NA.25

Properties

• Quality Level: 100
• 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

Description

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.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves