Rimegepant (BMS-927711) is a highly potent, oralcalcitoningene-related peptide (CGRP) receptor antagonist with aK_iof 0.027 nM and anIC₅₀of 0.14 nM for hCGRP receptor^[1].

Ki: 0.027 nM (CGRP receptor)^[1]
IC50: 0.14 nM (CGRP receptor)^[1]

Rimegepant (BMS-927711) is a full, competitive CGRP receptor antagonist with IC₅₀of 0.14±0.01 nM^[1].

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^[1]. 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)^[2].

534.56

Solid

C₂₈H₂₈F₂N₆O₃

1289023-67-1

Room temperature in continental US; may vary elsewhere.

DMSO : 10 mg/mL(18.71 mM;Need ultrasonic and warming)

Ethanol : 4.4 mg/mL(8.23 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 5% DMSO    40%PEG300   5%Tween-80   50% saline

  Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution
• 2.

  请依序添加每种溶剂： 10% EtOH    90%PEG300

  Solubility: ≥ 1 mg/mL (1.87 mM); Clear solution