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
结构式
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]-
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。