| Identification | Back Directory | [Name]
Rimegepant | [CAS]
1289023-67-1 | [Synonyms]
CS-2806
BHV-3000
BMS 92771
BMS 927711
BMS-927711
Rimegepant
BMS927711;BMS 927711
BMS-927711(Rimegepant)
RIMEGEPANT;BMS-927711;BMS927711;BMS 92771
(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
4-(2,3-Dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-1-piperidinecarboxylic acid (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl ester
1-Piperidinecarboxylic acid, 4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-, (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl ester | [Molecular Formula]
C28H28F2N6O3 | [MDL Number]
MFCD23098777 | [MOL File]
1289023-67-1.mol | [Molecular Weight]
534.56 |
| Chemical Properties | Back Directory | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
A crystalline solid | [pka]
12.03±0.20(Predicted) | [color ]
White to off-white | [InChIKey]
KRNAOFGYEFKHPB-ANJVHQHFSA-N | [SMILES]
N1(C(O[C@H]2C3=NC=CC=C3[C@@H](N)[C@H](C3=CC=CC(F)=C3F)CC2)=O)CCC(N2C3=CC=CN=C3NC2=O)CC1 |
| Hazard Information | Back Directory | [Description]
Rimegepant (Nurtec ODT)(FDA approved in February 2020) is an ODT available in a single strength of 75 mg for the acute treatment of migraine with or without aura in adults.No more than 75 mg should be taken in a 24-hour period. while there are no contraindications，concomitant administration with CYP3A4 inhibitors should be avoided.The most common adverse reaction is nausea, occurring in few patients (rimegepant PI, 2020). In clinical trials, a single 75-mg dose of rimegepant demonstrated superiority over placebo with regard to freedom from pain (21% in the rimegepant group vs.11% in the placebo group) and freedom from the most bothersome symptom (35% vs. 27%) at 2 hours post dose (Croop et al., 2019). Rimegepant is not approved for migraine prevention, although it is presently in late-stage clinical trials assessing it for that indication(NCT03732638,2020). | [Uses]
Rimegepant is an oral calcitonin gene-related peptide (CGRP) receptor antagonist used for the treatment of migraine. | [in vivo]
Rimegepant (BMS-927711) has good oral bioavailability in rat and cynomolgus monkey, attractive overall preclinical properties, and shows dose-dependent activity in a primate model of CGRP-induced facial blood flow[1]. The ratios of the mean AUC (0-24 h) values for Rimegepant (BMS-927711) (60, 100, and 300 mg/kg) in the DBS matrix, compare with plasma, are 0.5-0.6 across all doses in rats. Results from this study suggest a strong correlation of Rimegepant concentrations between rat plasma and rat blood (DBS)[2]. |
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