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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $50 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $162 | In Stock | |
25 mg | $333 | In Stock | |
50 mg | $495 | In Stock | |
100 mg | $719 | In Stock | |
500 mg | $1,490 | In Stock | |
1 mL x 10 mM (in DMSO) | $138 | In Stock |
Description | Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM. |
In vitro | BMS-927711 is a full, competitive CGRP receptor antagonist with IC50 of 0.14±0.01 nM. |
In vivo | The mean area under the curve (AUC) (0-24 h) ratios for BMS-927711 at dosages of 60, 100, and 300 mg/kg in the dried blood spot (DBS) matrix versus plasma range from 0.5-0.6 for all doses in rats, indicating a strong correlation between BMS-927711 concentrations in rat plasma and DBS. This study demonstrates that BMS-927711 possesses favorable oral bioavailability in both rats and cynomolgus monkeys, alongside promising preclinical attributes. Furthermore, it exhibits dose-dependent efficacy in a primate model of Calcitonin Gene-Related Peptide (CGRP)-induced facial blood flow, underscoring its potential therapeutic utility. |
Alias | BMS 927711, BMS-927711, BMS927711, BHV-3000 |
Molecular Weight | 534.56 |
Formula | C28H28F2N6O3 |
Cas No. | 1289023-67-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||
Solubility Information | DMSO: 50 mg/mL (93.53 mM) ![]() Ethanol: 10 mg/mL | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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