1197420-11-3

中文名称 Thieno[3,2-d]pyrimidin-4(3H)-one, 6-(4-chlorophenyl)-3-[4-[(3,3-difluoro-1-hydroxycyclobutyl)methoxy]-3-methoxyphenyl]-

英文名称 Thieno[3,2-d]pyrimidin-4(3H)-one, 6-(4-chlorophenyl)-3-[4-[(3,3-difluoro-1-hydroxycyclobutyl)methoxy]-3-methoxyphenyl]-

CAS 1197420-11-3

分子式 C24H19ClF2N2O4S

分子量 504.93

MOL 文件 1197420-11-3.mol

1197420-11-3 结构式

基本信息物理化学性质应用领域常见问题列表

基本信息

中文别名

化合物 T26860

英文别名

BMS 814580
Thieno[3,2-d]pyrimidin-4(3H)-one, 6-(4-chlorophenyl)-3-[4-[(3,3-difluoro-1-hydroxycyclobutyl)methoxy]-3-methoxyphenyl]-

物理化学性质

沸点691.9±65.0 °C(Predicted)

密度1.49±0.1 g/cm3(Predicted)

酸度系数(pKa)12.36±0.40(Predicted)

应用领域

用途一

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 demonstrates reduction in feeding and body weight in rats and mice.

常见问题列表

概述

BMS-814580 是一种具有口服活性的、高效的 MCHR1 抑制剂，Ki 值为 16.9 nM。 BMS-814580 具有抗肥胖活性。