GPR40 Agonist II

Not available outside of the UK & Ireland.

General description

A cell-permeable alkynedihydrocinnamic acid that acts as a potent GPR40/FFA1 agonist (EC₅₀ = 40.7 nM in inducing Ca²⁺ mobilization in hFFA1-expressing 1321N1 cells) with >100-fold selectivity over GPR43/FFA2, GPR41/FFA3, and a panel of 56 other receptors, ion channels, and transporters. Reported to enhance 12 mM glucose-induced insulin secretion from rat INS-1E β-cells (by 34% at 10 µM) and exhibit good aqueous solubility (199 µM in PBS at pH 7.4), as well as chemical and metabolic stability.

A cell-permeable alkynedihydrocinnamic acid that acts as a potent GPR40/FFA1 agonist (EC₅₀ = 40.7 nM in inducing Ca²⁺ mobilization in hFFA1-expressing 1321N1 cells) with >100-fold selectivity over GPR43/FFA2, GPR41/FFA3, and a panel of 56 other receptors, ion channels, and transporters. Reported to enhance 12 mM glucose-induced insulin secretion from rat INS-1E β-cells (by 34% at 10 µM) and exhibit good aqueous solubility (199 µM in PBS at pH 7.4), as well as chemical (0.1% degradation after 12 days in PBS at 37 °C) and metabolic (3% metabolization by human liver S9 stability test) stability.

Legal Information

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

Other Notes

Christiansen, E., et al. 2011, J. Med. Chem.54, 6691.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)