Rimegepant, also known as BMS-927711, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist with a Ki value of 0.027 nM. Rimegepant has shown in vivo efficacy without vasoconstriction effect. BMS-927711 is superior to placebo at several different doses (75 mg, 150 mg, and 300 mg) and has an excellent tolerability profile. The compound is unstable in solutions, freshly prepared is recommended.
Molecular Weight | 534.56 |
Formula | C28H28F2N6O3 |
CAS Number | 1289023-67-1 |
Solubility (25°C) | DMSO 9 mg/mL Ethanol 9 mg/mL |
Storage | -20°C |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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Adrenomedullin (AM) (22-52), human
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