BMS927711 是一种有效的降钙素基因相关肽 (CGRP) 受体拮抗剂,其 Ki=0.027 nM,IC50=0.14 nM。
产品描述
BMS-927711 is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.
体外活性
BMS-927711 is a full, competitive CGRP receptor antagonist with IC50 of 0.14±0.01 nM.
体内活性
The ratios of the mean AUC (0-24 h) values for BMS-927711 (60, 100, and 300 mg/kg) in the DBS matrix, compare with plasma, are 0.5-0.6 across all doses in rats. Results from this study suggest a strong correlation of BMS-927711 concentrations between rat plasma and rat blood (DBS).BMS-927711 has good oral bioavailability in rat and cynomolgus monkey, attractive overall preclinical properties, and shows dose-dependent activity in a primate model of CGRP-induced facial blood flow
Cas No.
1289023-67-1
分子式
C28H28F2N6O3
分子量
534.568
别名
BHV-3000;BMS927711;BMS 927711;BMS-927711
储存和溶解度
DMSO:10 mg/mL
Ethanol:10 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years