GPR40 Agonist

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.

Packaged under inert gas

Toxicity: Standard Handling (A)

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

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

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