Rimegepant (sulfate hydrate)

Rimegepant (BMS-927711) sulfate hydrate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor. Rimegepant sulfate hydrate can be used for migraine research[1][2][3].

Product Specifications

CAS Number

[1374024-48-2]

Product Name Alternative

BMS-927711 (sulfate hydrate) ; BHV-3000 (sulfate hydrate)

UNSPSC

12352005

Target

CGRP Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Purity

99.48

Solubility

DMSO : 7 mg/mL (ultrasonic)

Smiles

O=S(O)(O)=O.O=C1N(C2CCN(CC2)C(O[C@H]3C4=NC=CC=C4[C@H]([C@H](C5=C(C(F)=CC=C5)F)CC3)N)=O)C6=CC=CN=C6N1.O.[0.5].[1.5]

Molecular Formula

C28H28F2N6O3.1/2H2O4S.3/2H2O

Molecular Weight

610.26

References & Citations

[1]Blair HA. Rimegepant: A Review in the Acute Treatment and Preventive Treatment of Migraine. CNS Drugs. 2023 Mar;37 (3) :255-265. |[2]Vladimir Coric, et al. Dual treatment of migraine. WO2022251752. 2022-12-29.|[3]Luo G, et al. Discovery of (5S,6S,9R) -5-amino-6- (2,3-difluorophenyl) -6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl) piperidine-1-carboxylate (BMS-927711) : an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine. J Med Chem. 2012 Dec 13;55 (23) :10644-51.