Rimegepant (hemisulfate)

Rimegepant (BMS-927711) hemisulfate 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 hemisulfate can be used for migraine research[1][2][3].

Product Specifications

CAS Number

[1642783-82-1]

Product Name Alternative

BMS-927711 (hemisulfate) ; BHV-3000 (hemisulfate)

UNSPSC

12352005

Target

CGRP Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

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.[1/2]

Molecular Formula

C28H28F2N6O3·1/2H2SO4

Molecular Weight

583.60

References & Citations

[1]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.|[2]Vladimir Coric, et al. Dual treatment of migraine. WO2022251752. 2022-12-29.|[3]Blair HA. Rimegepant: A Review in the Acute Treatment and Preventive Treatment of Migraine. CNS Drugs. 2023 Mar;37 (3) :255-265. doi: 10.1007/s40263-023-00988-8. Epub 2023 Feb 4. Erratum in: CNS Drugs. 2023 Jul;37 (7) :661.