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Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 47 € | In Stock | |
5 mg | 93 € | In Stock | |
10 mg | 153 € | In Stock | |
25 mg | 254 € | 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. |
Targets&IC50 | CGRP receptor:0.14 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, BMS927711, BMS 927711, BHV-3000 |
Molecular Weight | 534.56 |
Formula | C28H28F2N6O3 |
Cas No. | 1289023-67-1 |
Smiles | N[C@H]1[C@@H](CC[C@@H](OC(=O)N2CCC(CC2)n2c3cccnc3[nH]c2=O)c2ncccc12)c1cccc(F)c1F |
Relative Density. | 1.45 g/cm3 (Predicted) |
Storage | keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (93.53 mM) Ethanol: <1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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