GPR40 Agonist III

A cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC₅₀ = 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Christiansen, E., et al. 2013. J. Med. Chem.56, 982.

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

Toxicity: Standard Handling (A)