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CAS No. : 1289023-67-1
MCE 国际站:Rimegepant
产品活性:Rimegepant (BMS-927711) 是一种有效的降钙素基因相关肽 (CGRP) 受体拮抗剂,对 hCGRP 受体的 Ki 为 0.027 nM,IC50 为 0.14 nM。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:CGRP Receptor
In Vitro: Rimegepant (BMS-927711) is a full, competitive CGRP receptor antagonist with IC50 of 0.14±0.01 nM.
In Vivo: Rimegepant (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. The ratios of the mean AUC (0-24 h) values for Rimegepant (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 Rimegepant concentrations between rat plasma and rat blood (DBS).
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