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Purity: ≥98%
Rimegepant (formerly known as BMS-927711; Nurtec ODT) is a highly potent, selective, orally bioavailable, cometitive calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM. In 2020, Rimegepant received approval as a medicine for the acute management of adult episodic migraines with or without aura as well as for the prophylactic treatment of adult migraines. It has been shown that calcitonin gene-related peptide (CGRP) receptor antagonists are clinically effective in treating acute migraines. In addition to having attractive overall preclinical properties and good oral bioavailability in rats and cynomolgus monkeys, BMS-927711 also demonstrates dose-dependent activity in a primate model of CGRP-induced facial blood flow. At three different doses (75 mg, 150 mg, and 300 mg), BMS-927711 outperforms a placebo and has an excellent tolerability profile. Trials for BMS-927711 are currently in phase II.
| Targets |
CGRP receptor ( Ki = 0.027 nM )
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| ln Vitro |
Rimegepant (BMS-927711, BHV-3000) is a potent, competitive, and selective antagonist of the human calcitonin gene-related peptide (CGRP) receptor with ki of 0.027 nM.
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| References |
| Molecular Formula |
C28H28F2N6O3
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| Molecular Weight |
534.57
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| Exact Mass |
534.22
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| Elemental Analysis |
C, 62.91; H, 5.28; F, 7.11; N, 15.72; O, 8.98
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| CAS # |
1289023-67-1
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| Related CAS # |
1289023-67-1; 1642783-82-1 (0.5 sulfate); 1374024-48-2 (0.5 sulfate 1.5 hydrate); 2377164-85-5 (0.5 sulfate 3 hydrate)
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| Appearance |
Solid powder
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| SMILES |
C1C[C@H](C2=C(C=CC=N2)[C@H]([C@@H]1C3=C(C(=CC=C3)F)F)N)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6
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| InChi Key |
KRNAOFGYEFKHPB-ANJVHQHFSA-N
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| InChi Code |
InChI=1S/C28H28F2N6O3/c29-20-6-1-4-17(23(20)30)18-8-9-22(25-19(24(18)31)5-2-12-32-25)39-28(38)35-14-10-16(11-15-35)36-21-7-3-13-33-26(21)34-27(36)37/h1-7,12-13,16,18,22,24H,8-11,14-15,31H2,(H,33,34,37)/t18-,22+,24-/m0/s1
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| Chemical Name |
[(5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl] 4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
5%DMSO + Corn oil: 5.0mg/ml (9.35mM) (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8707 mL | 9.3533 mL | 18.7066 mL | |
| 5 mM | 0.3741 mL | 1.8707 mL | 3.7413 mL | |
| 10 mM | 0.1871 mL | 0.9353 mL | 1.8707 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05207865 | Active Recruiting |
Drug: Rimegepant | Migraine Episodic Migraine Phonophobia |
Pfizer | March 15, 2022 | Phase 4 |
| NCT05399485 | Active Recruiting |
Drug: Rimegepant Drug: Placebo |
Migraine | Pfizer | August 9, 2022 | Phase 3 |
| NCT05399459 | Active Recruiting |
Drug: Rimegepant 25 MG Drug: Rimegepant 75 MG |
Migraine | Pfizer | August 9, 2022 | Phase 3 |
| NCT05371652 | Active Recruiting |
Drug: Rimegepant 75mg Orally Disintegrating Tablets (ODT) |
Acute Migraine | Pfizer | May 19, 2022 | Phase 3 |
| NCT05509400 | Recruiting | Drug: Rimegepant Drug: Placebo |
Migraine | Pfizer | October 18, 2022 | Phase 4 |
Products are for research use only; We do not sell to patients
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