AMG 837 hemicalcium
AMG 837 calcium salt
AMG 837 hemicalcium salt
(βS)-β-1-Propyn-1-yl-4-[[4'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]methoxy]benzenepropanoic acid hemicalcium salt
AMG 837 Hemicalcium Salt is used in the synthetic preparation of a novel GPR40 receptor agonist, AMG 837 (A614410). GPR40 is a polyunsaturated fatty acid receptor that is involved with many systemic effects, which are beneficial for metabolic and inflammatory diseases. GPR40 has also been implicated as a target for treating obesity.
in vivo
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 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo[1].
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F?=?84%) and a total plasma Cmax of 1.4 μM[1].
Animal Model:
8-week old Zucker Fatty Rats[1]
Dosage:
0.03, 0.1, 0.3 mg/kg
Administration:
Oral gavage once daily for 21 days
Result:
Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively.
Increased insulin levels in the mid- and high-dose groups.
Not affected body weights during the 21-day treatment.
Animal Model:
8-week old Sprague-Dawley rats[1]
Dosage:
0.03, 0.1, 0.3 mg/kg
Administration:
A single p.o. administration
Result:
Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.
