Rimegepant sulfate hydrate
Based on 12 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.56%
- CAS No.: 1374024-48-2
- Formula: C28H32F2N6O3.1/2H2O4S.3/2H2O
- Molecular Weight:610.26
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Rimegepant sulfate hydrate
More- Nature. 2025 Apr;640(8059):802-810. [Abstract]
- Lancet Neurol. 2022 Mar;21(3):284-294. [Abstract]
- Cell. 2025 Nov 26;188(24):6754-6773.e29. [Abstract]
- Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
- J Immunother Cancer. 2026 May 8;14(5):e013958. [Abstract]
- Free Radic Biol Med. 2025 Dec 24:245:18-29. [Abstract]
- Br J Pharmacol. 2024 Jan;181(1):142-161. [Abstract]
- Ann Neurol. 2020 Oct;88(4):771-784. [Abstract]
- Vascul Pharmacol. 2017 Mar:90:36-43. [Abstract]
- Pharmacology. 2019;104(5-6):332-341. [Abstract]
- bioRxiv. 2026 May 22:2026.05.20.725748. [Abstract]
- bioRxiv. 2024 Mar 8:2024.03.04.583209. [Abstract]
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Histological Imaging/Staining
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In Vivo Efficacy Study
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Flow Cytometry
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In Vivo Efficacy Study
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Histological Imaging/Staining
Biological Activity
| Species | Dose | Route | Plasma Concentration |
|---|---|---|---|
| Mice[3] | 12.84 mg/kg | p.o. | 562 ng/mL |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1374024-48-2
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Appearance Solid
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Molecular Weight 610.26
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Formula C28H32F2N6O3.1/2H2O4S.3/2H2O
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Color White to off-white
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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]
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Synonyms
BMS-927711 sulfate hydrate; BHV-3000 sulfate hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (12)
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Journal Impact Factor
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Most Recent
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Nature
2025 Apr;640(8059):802-810. PMID: 39972142
Rimegepant sulfate hydrate purchased from MedChemExpress. Usage Cited in: Nature. 2025 Apr;640(8059):802-810. [Abstract]
Representative images of MNU-induced dysplasia from CNO-treated mice with or without Rimegepant administration were presented. CNO-activated mice treated with a diet containing Rimegepant (a CGRP antagonist; 10 mg/kg; mixed into the AIN-76A mouse chow) showed reduced MNU-induced tumour development compared with the untreated controls.
Rimegepant sulfate hydrate purchased from MedChemExpress. Usage Cited in: Nature. 2025 Apr;640(8059):802-810. [Abstract]
Representative images of syngeneic orthotopic tumours from CNO-treated mice with or without Rimegepant (a CGRP antagonist; 10 mg/kg; mixed into the AIN-76A mouse chow) administration were shown. Nociceptive neuronal activation resulted in significantly increased tumour volume, which was inhibited by Rimegepant treatment.
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Lancet Neurol
Calcitonin gene-related peptide-targeting drugs for migraine: how pharmacology might inform treatment decisions. [Abstract]2022 Mar;21(3):284-294. PMID: 35093196 -
Cell
2025 Nov 26;188(24):6754-6773.e29. PMID: 41138728 -
Cell Metab
Cancer cells co-opt nociceptive nerves to thrive in nutrient-poor environments and upon nutrient-starvation therapies. [Abstract]2022 Dec 6;34(12):1999-2017.e10. PMID: 36395769
Rimegepant sulfate hydrate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
Treated OSCCPDEs with TG CM significantly increased the proportion of Ki67+ cancer cells under low-glucose culture and upon 2-DG treatment, which was antagonized by Rimegepant via antagonism of CGRP-CLR signaling.
Rimegepant sulfate hydrate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
In vitro Cal27 cell growth of indicated cancer cells upon Rimegepant treatment for 48 hrs (n=4 biological replicates per group).
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J Immunother Cancer
Sensory neuron-derived CCL5 orchestrates an immunosuppressive niche via regulatory T cells to fuel head and neck tumor progression. [Abstract]2026 May 8;14(5):e013958. PMID: 42103358 -
Free Radic Biol Med
Oxidative stress impairs the expansion of regulatory T cells in active vitiligo via dysregulated CGRP-RAMP1-Gαi3 signaling. [Abstract]2025 Dec 24:245:18-29. PMID: 41453541
Rimegepant sulfate hydrate purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Dec 24:245:18-29. [Abstract]
Reduced proliferative responsiveness of Tregs isolated from patients with active vitiligo to CGRP was observed. CD4 + CD25 high CD127 dim Tregs were sorted by flow cytometry and cultured for 72 h in the presence of Rimegepant (1 μM). DMSO was used as the vehicle control. Representative scatter plots of Tregs from healthy controls (upper panels) and from patients with active vitiligo (lower panels) were shown.
Rimegepant sulfate hydrate purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Dec 24:245:18-29. [Abstract]
Effects of Rimegepant (0.2 mg/mouse/day; oral gavage; three times weekly for 3 weeks) on depigmentation in the tail skin of vitiligo model mice were investigated. Representative macroscopic and Wood's lamp images of tail skin from each group were shown. White arrows indicated depigmented areas, and quantification of depigmented areas was shown on the right. Rimegepant partially reversed CGRP-induced vitiligo progression.
Rimegepant sulfate hydrate purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Dec 24:245:18-29. [Abstract]
X-gal staining and immunofluorescence were performed on tail skin sections from each group. Upper panels: X-gal staining visualized MCs (black arrows); black dashed lines indicated borders between depigmented and normally pigmented areas. Lower panels: Immunofluorescence staining of FOXP3+ Tregs (green) with nuclei labeled by DAPI (blue); white dashed lines denoted the dermal-epidermal junction, and white arrows indicated FOXP3+ Tregs. Rimegepant (0.2 mg/mouse/day; oral gavage; three times weekly for 3 weeks) partially reversed CGRP-induced vitiligo progression and restored Treg numbers.
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Br J Pharmacol
2024 Jan;181(1):142-161. PMID: 37580864 -
Ann Neurol
Anti-migraine Calcitonin Gene-Related Peptide Receptor Antagonists Worsen Cerebral Ischemic Outcome in Mice. [Abstract]2020 Oct;88(4):771-784. PMID: 32583883 -
Vascul Pharmacol
Binding and functional pharmacological characteristics of gepant-type antagonists in rat brain and mesenteric arteries. [Abstract]2017 Mar:90:36-43. PMID: 28192258 -
Pharmacology
The Presence of Calcitonin Gene-Related Peptide and Its Receptors in Rat, Pig and Human Brain: Species Differences in Calcitonin Gene-Related Peptide Pharmacology. [Abstract]2019;104(5-6):332-341. PMID: 31484177 -
bioRxiv
2026 May 22:2026.05.20.725748. PMID: 42239358 -
bioRxiv
Nociceptive neurons interact directly with gastric cancer cells via a CGRP/Ramp1 axis to promote tumor progression. [Abstract]2024 Mar 8:2024.03.04.583209. PMID: 38496544
Solvent & Solubility
DMSO : 7 mg/mL (11.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Blair HA. Rimegepant: A Review in the Acute Treatment and Preventive Treatment of Migraine. CNS Drugs. 2023 Mar;37(3):255-265. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6386 mL | 8.1932 mL | 16.3865 mL | 40.9661 mL |
| 5 mM | 0.3277 mL | 1.6386 mL | 3.2773 mL | 8.1932 mL | |
| 10 mM | 0.1639 mL | 0.8193 mL | 1.6386 mL | 4.0966 mL |