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LY2922470 is an agonist of free fatty acid receptor 1 (FFAR1/GPR40).1 It induces calcium flux in HEK293 cells expressing FFAR1/GPR40 (EC50s = 7, 1, and 3 nM for the human, mouse, and rat receptor, respectively). LY2922470 (30 mg/kg) increases blood levels of glucagon-like peptide 1 (GLP-1) in fasted mice. It also decreases cerebral infarct area in a mouse model of ischemia-reperfusion injury induced by middle cerebral artery occlusion (MCAO) when administered at doses of 10, 20, or 40 mg/kg.2
WARNING This product is not for human or veterinary use.
1. The discovery, preclinical, and early clinical development of potent and selective GPR40 agonists for the treatment of type 2 diabetes mellitus (LY2881835, LY2922083, and LY2922470). J. Med. Chem. 59(24), 10891-10916 (2016).
2. G protein-