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 |