BMS-814580 is a Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor with potential anti-obesity property. BMS-814580 exhibits potent binding affinity (Ki = 17 nM) for human MCHR1. BMS-814580 is a potent and selective functional antagonist (Kb = 117 nM) of human MCHR1. In a FLIPR-based assay BMS-814580 exhibiting no activity against MCHR2 at 10 μM. BMS-814580 also exhibits potent binding affinities for cynomolgus monkey and rat MCHR1 (Ki of 4.9 and 11.5 nM, respectively). MCHR1 antagonist displays reduction in feeding and body weight in rats and mice. References: Ahmad S, Washburn WN, Hernandez AS, Bisaha S, Ngu K, Wang W, Pelleymounter MA, Longhi D, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas MA, Glick S, Godonis H, Harvey S, Zhang H, Gemzik B, Janovitz EB, Huang C, Zhang L, Robl JA, Murphy BJ. Synthesis and Anti-obesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphen yl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor-1 (MCHR1) Inhibitor. J Med Chem. 2016 Aug 26. [Epub ahead of print] PubMed PMID: 27564419.

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CAS：1197420-11-3