371706

GPR40 Agonist

The GPR40 Agonist, also referenced under CAS 885101-89-3, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• Synonym(s): GPR40 Agonist, 3-(4-(((3-(Phenoxy)phenyl)methyl)amino)phenyl)propanoic acid, FFA1 Agonist I, Free Fatty Acid Receptor 1 Agonist I
• Empirical Formula (Hill Notation): C₂₂H₂₁NO₃
• CAS Number: 885101-89-3
• Molecular Weight: 347.41
• MDL number: MFCD09753282
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light yellow
• solubility: DMSO: 40 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• 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

General description

A cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GPR40 (EC₅₀ ~50 nM) with much reduced activity towards family members GPR120 (EC₅₀ ~3.5 µM), GPR41/GPR43 (EC₅₀ >50 µM), as well as a panel of eight other fatty acid and prostaglandin receptors. Shown to induces GPR40-dependent Ca²⁺ mobilization in HEK-293 cells and potentiate glucose-stimulated insulin secretion in MIN6 cells. Reported to exhibit an in vivo half-life of ≥5.3 hr. in rat (p.o. or i.v.) with a bioavailability of 65% and a clearance of 24.9 ml/min/kg.

A cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40 (EC₅₀ ~50 nM) with much reduced activity towards family members GRP120 (EC₅₀ ~3.5 µM), GRP41/GRP43 (EC₅₀ >50 µM), as well as a panel of eight other fatty acid and prostaglandin receptors. Shown to induces GPR40-dependent Ca²⁺ mobilization in HEK-293 cells and potentiate glucose-stimulated insulin secretion in MIN6 cells. Reported to exhibit an in vivo half-life of ≥5.3 hr. in rat (p.o. or i.v.) with a bioavailability of 65% and a clearance of 24.9 ml/min/kg.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

McKeown, S C., et al. 2007. Bioorg. Med. Chem. Lett.17, 1584.
Briscoe, C. P., et al. 2006. Br. J. Pharmacol.148, 619.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3