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MedKoo Cat#: 330049 | Name: Rimegepant sulfate hydrate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Rimegepant, also known as BMS-927711 and BHV-3000, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraines. 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.

Chemical Structure

Rimegepant sulfate hydrate
Rimegepant sulfate hydrate
CAS#1374024-48-2 (0.5 sulfate 1.5 hydrate)

Theoretical Analysis

MedKoo Cat#: 330049

Name: Rimegepant sulfate hydrate

CAS#: 1374024-48-2 (0.5 sulfate 1.5 hydrate)

Chemical Formula: C56H64F4N12O13S

Exact Mass:

Molecular Weight: 1221.25

Elemental Analysis: C, 55.08; H, 5.28; F, 6.22; N, 13.76; O, 17.03; S, 2.63

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1289023-67-1 (free base) 1374024-48-2 (0.5 sulfate 1.5 hydrate) 1642783-82-1 (0.5 sulfate) 2377164-85-5 (0.5 sulfate 3 hydrate)
Synonym
Rimegepant sulfate, BHV-3000; BHV 3000; BHV3000; BMS-927711; BMS 927711; BMS927711; Rimegepant;
IUPAC/Chemical Name
Di((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), monosulfate, trihydrate
InChi Key
SOGUOEZRYKUOHR-CQZKMDJHSA-N
InChi Code
InChI=1S/2C28H28F2N6O3.H2O4S.3H2O/c2*29-20-6-1-4-17(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;1-5(2,3)4;;;/h2*1-7,12-13,16,18,22,24H,8-11,14-15,31H2,(H,33,34,37);(H2,1,2,3,4);3*1H2/t2*18-,22+,24-;;;;/m00..../s1
SMILES Code
O=C(N1CCC(N(C2=CC=CN=C2N3)C3=O)CC1)O[C@@H]4CC[C@@H](C5=CC=CC(F)=C5F)[C@H](N)C6=CC=CN=C64.O=C(N7CCC(N(C8=CC=CN=C8N9)C9=O)CC7)O[C@@H]%10CC[C@@H](C%11=CC=CC(F)=C%11F)[C@H](N)C%12=CC=CN=C%12%10.O=S(O)(O)=O.[H]O[H].[H]O[H].[H]O[H]
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 1,221.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Pan KS, Siow A, Hay DL, Walker CS. Antagonism of CGRP Signaling by Rimegepant at Two Receptors. Front Pharmacol. 2020 Aug 20;11:1240. doi: 10.3389/fphar.2020.01240. PMID: 32973499; PMCID: PMC7468408. 2: DeFalco AP, Lazim R, Cope NE. Rimegepant Orally Disintegrating Tablet for Acute Migraine Treatment: A Review. Ann Pharmacother. 2020 Sep 10:1060028020954800. doi: 10.1177/1060028020954800. Epub ahead of print. PMID: 32909437. 3: Rimegepant (Nurtec ODT) for Acute Treatment of Migraine. JAMA. 2020 Sep 1;324(9):890-891. doi: 10.1001/jama.2020.8493. PMID: 32870296. 4: Berman G, Croop R, Kudrow D, Halverson P, Lovegren M, Thiry AC, Conway CM, Coric V, Lipton RB. Safety of Rimegepant, an Oral CGRP Receptor Antagonist, Plus CGRP Monoclonal Antibodies for Migraine. Headache. 2020 Aug 16;60(8):1734–42. doi: 10.1111/head.13930. Epub ahead of print. PMID: 32799325; PMCID: PMC7496574. 5: Doty EG, Krege JH, Pohl G, Case M, Dowsett SA, Tepper SJ. Pain Freedom at 2 to 8 Hours With Lasmiditan: A Comparison With Rimegepant and Ubrogepant. Headache. 2020 Jul 22. doi: 10.1111/head.13899. Epub ahead of print. PMID: 32700321. 6: Gasparini S, Torino C, Branca D, Ferlazzo E, Aguglia U. Testing rimegepant for migraine-time to revise the trial design? Lancet. 2020 Jun 20;395(10241):1901. doi: 10.1016/S0140-6736(20)30241-5. PMID: 32563366. 7: Croop R, Goadsby PJ, Stock DA, Lipton RB. Testing rimegepant for migraine- time to revise the trial design? - Authors' reply. Lancet. 2020 Jun 20;395(10241):1901-1902. doi: 10.1016/S0140-6736(20)30231-2. PMID: 32563365. 8: Rimegepant (Nurtec ODT) for acute treatment of migraine. Med Lett Drugs Ther. 2020 May 4;62(1597):70-72. PMID: 32555113. 9: Scott LJ. Rimegepant: First Approval. Drugs. 2020 May;80(7):741-746. doi: 10.1007/s40265-020-01301-3. PMID: 32270407. 10: Gao B, Yang Y, Wang Z, Sun Y, Chen Z, Zhu Y, Wang Z. Efficacy and Safety of Rimegepant for the Acute Treatment of Migraine: Evidence From Randomized Controlled Trials. Front Pharmacol. 2020 Jan 24;10:1577. doi: 10.3389/fphar.2019.01577. PMID: 32038251; PMCID: PMC6992660. 11: McCarthy L. Oral rimegepant increased freedom from pain and from most bothersome symptom at 2 h in acute migraine. Ann Intern Med. 2019 Nov 19;171(10):JC59. doi: 10.7326/ACPJ201911190-059. PMID: 31739342. 12: McCarthy L. Orally disintegrating rimegepant increased freedom from pain and from most bothersome symptom at 2 h in acute migraine. Ann Intern Med. 2019 Nov 19;171(10):JC58. doi: 10.7326/ACPJ201911190-058. PMID: 31739341. 13: Ju C, Spiegel R, Radecki R, Swaminathan AK. Rimegepant in the Treatment of Migraine Headache: The Importance of Comparator Treatments: November 2019 Annals of Emergency Medicine Journal Club. Ann Emerg Med. 2019 Nov;74(5):721-723. doi: 10.1016/j.annemergmed.2019.09.014. PMID: 31668246. 14: Edvinsson L. Rimegepant oral disintegrating tablet for migraine. Lancet. 2019 Aug 31;394(10200):711-712. doi: 10.1016/S0140-6736(19)31611-3. Epub 2019 Jul 13. PMID: 31311675. 15: Croop R, Goadsby PJ, Stock DA, Conway CM, Forshaw M, Stock EG, Coric V, Lipton RB. Efficacy, safety, and tolerability of rimegepant orally disintegrating tablet for the acute treatment of migraine: a randomised, phase 3, double-blind, placebo-controlled trial. Lancet. 2019 Aug 31;394(10200):737-745. doi: 10.1016/S0140-6736(19)31606-X. Epub 2019 Jul 13. PMID: 31311674. 16: Lipton RB, Croop R, Stock EG, Stock DA, Morris BA, Frost M, Dubowchik GM, Conway CM, Coric V, Goadsby PJ. Rimegepant, an Oral Calcitonin Gene-Related Peptide Receptor Antagonist, for Migraine. N Engl J Med. 2019 Jul 11;381(2):142-149. doi: 10.1056/NEJMoa1811090. PMID: 31291516.

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