PeptideDB

BMS-814580

CAS: 1197420-11-3 F: C24H19ClF2N2O4S W: 504.93

BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows
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Bioactivity BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities[1].
Target Ki: 16.9 nM (MCHR1)
Invitro BMS-814580 (3.0 μM; 10 min) shows stability with 90%, 95% and 100% remaining in human, rat and mouse liver microsomes, respectively[1].BMS-814580 displays modest in vitro ion channel inhibition of 43%, 21%, and 15%, respectively, for hERG, Na (4 Hz), and L-type Ca channels at 10 μM[1].
In Vivo BMS-814580 (0-3 mg/kg; p.o.; once daily for 28 days) shows antiobesity activities in rats[1]. Animal Model:
Name BMS-814580
CAS 1197420-11-3
Formula C24H19ClF2N2O4S
Molar Mass 504.93
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Ahmad S, et al. Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1