AMG 837

AMG 837 is a partial agonist of free fatty acid receptor 1 (FFAR1/GPR40).¹ It induces calcium mobilization in CHO cells expressing FFAR1/GPR40 but not FFAR2/GPR43, FFAR3/GPR41, or FFAR4/GPR120 (EC₅₀s = 0.0135, >10, >10, and >10 µM, respectively).^1,2 AMG 837 induces insulin secretion in MIN6 pancreatic β-cells and isolated mouse islets (EC₅₀s = 0.0048 and 0.142 µM, respectively).^1,2 It decreases plasma glucose levels and increases plasma levels of insulin in Zucker fa/fa rats when administered at doses of 0.3, 1, and 3 mg/kg.² AMG 837 (100 mg/kg) also decreases plasma glucose and increases plasma insulin levels in a mouse model of diabetes induced by a high-fat diet and streptozotocin (STZ; Item No. 13104).³

WARNING This product is not for human or veterinary use.

1. Houze, J.B., Zhu, L., Sun, Y., et al. AMG 837: A potent, orally bioavailable GPR40 agonist. Bioorg. Med. Chem. Lett 22(2), 1267-1270 (2012).

2. Lin, D.C.-H., Zhang, J., Zhuang, R., et al. AMG 837: A novel GPR40/FFA₁ agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One 6(11), e27270 (2011).

3. Luo, J., Swaminath, G., Brown, S.P., et al. A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents. PLoS One 7(10), e46300 (2012).