AMG 837 (calcium hydrate)

AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [³H]AMG 837 binding at the human FFA1 receptor with a pIC₅₀ of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents^[1][2][3]. AMG 837 (calcium hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target:pIC50: 8.13 (FFA1)^[3] In Vitro: AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC₅₀ of 142±20 nM on islets isolated from mice^[1].
AMG 837 stimulates Ca²⁺ flux with the EC₅₀s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively^[1]. In Vivo: AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo^[1].
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats^[1].
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma C_max of 1.4 μM^[1].