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
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
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
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