Art. -Nr.: HY-15498

Rimegepant

(Synonyms: BMS-927711; BHV-3000)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

Rimegepant (BMS-927711; BHV-3000) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC₅₀ of 8.01 and a K_i of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.99%
CAS. Nr.: 1289023-67-1
Formel: C₂₈H₂₈F₂N₆O₃
Molecular Weight:534.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Rimegepant Chemical Structure

CAS. Nr.: 1289023-67-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
SK-N-MC	EC₅₀	0.14 nM Compound: 8, BMS-927711	Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assay Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 15 mins prior to CGRP challenge measured after 30 mins by HTRF assay	[PMID: 23153230]

In Vitro

Rimegepant (10 μM; 15 min) antagonizes cAMP production at rat CGRP, AMY₁, and AMY₃ receptors with apparent pA₂ values of 6.41, 6.43-5.73, and 6.45 respectively, but shows no quantifiable activity at other rat calcitonin family receptors^[1].
Rimegepant (10 μM; 15 min) antagonizes cAMP production at mouse CGRP receptors with an apparent pA₂ of 6.89, shows weak, inconsistent activity at mouse AMY₁ receptors, and has no quantifiable activity at other mouse calcitonin family receptors^[1].
Rimegepant (tested across a concentration range; 15 min) inhibits cAMP production at human CGRP receptors with a pIC₅₀ of 8.01, and at human AMY₁ receptors with pIC₅₀ values of 6.25 (human-αCGRP agonist) and 5.66 (human-amylin agonist)^[1].
Rimegepant (tested at concentrations enabling apparent pA₂ determination; 15 min) antagonizes cAMP production at human CGRP receptors with apparent pA₂ values of 9.56 (human-αCGRP) and 9.34 (human-βCGRP), and at human AMY₁ receptors with apparent pA₂ values of 8.07 (human-αCGRP) and 7.48 (human-amylin), but shows no quantifiable activity at human AM₁ or AM₂ receptors^[1].
Rimegepant (compound 8) potently binds to the human CGRP receptor in SK-N-MC cell membranes with a K_i of 0.027 nM and a protein-adjusted K_i of 0.39 nM^[2].
Rimegepant acts as a full, competitive antagonist of CGRP-stimulated cAMP production in SK-N-MC cells with an IC₅₀ of 0.14 nM^[2].
Rimegepant (BMS-927711/compound 8) has improved human liver microsomal stability with a half-life of 83 min^[2].
Rimegepant shows low inhibition of human CYP isoforms, with an IC₅₀ of 17 μM for CYP3A4 and IC₅₀ ≥20 μM for all other tested isoforms^[2].
Rimegepant exhibits no significant off-target liabilities in a panel of 45 receptor, ion channel binding, and enzyme activity assays^[2].
Rimegepant (10-30 μM) causes less than 30% inhibition of the hERG potassium channel at 10 and 30 μM and has no significant effect on L-type sodium or calcium channels in HEK-293 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	Plasma Concentration
Rat^[2]	7 mg/kg	s.c.	400 nM

In Vivo

Rimegepant (12.84 mg/kg; p.o.; single dose, daily for 7 days) administered orally at 12.84 mg/kg reaches measurable contents in mouse plasma, dura mater, TG, parietal brain cortex, and hypothalamus, with peak tissue levels at 3 hours post-single dose, and shows only minimal accumulation in the parietal brain cortex with chronic daily dosing^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57Bl/6J (adult male, 25-30 g)^[3]
Dosage:

12.84 mg/kg (single dose); 12.84 mg/kg (chronic 7-day dosing)
Administration:

p.o.; single dose; daily for 7 days
Result:

Reached a peak plasma concentration of 562 pg/µl at 3 hours post-single dose.
Reached a peak trigeminal ganglion (TG) content of 160 pg/mg at 3 hours post-single dose, with a flattened, prolonged increase compared to plasma.
Reached a peak parietal brain cortex content of 123 pg/mg at 3 hours post-single dose, with a temporal pattern similar to the TG.
Had lower drug contents in dura mater than corresponding plasma concentrations at 3 hours post-single dose.
Reached hypothalamus contents comparable to the TG at 3 hours post-single dose.
Had higher parietal brain cortex contents at 6 hours after the final chronic dose than levels measured 6 hours after a single dose.

Chemical Information

CAS. Nr. 1289023-67-1
Appearance Solid
Molecular Weight 534.56
Formel C₂₈H₂₈F₂N₆O₃
Color White to off-white
SMILES

N[C@H]1[C@H](C2=C(F)C(F)=CC=C2)CC[C@@H](OC(N3CCC(N4C(C=CC=N5)=C5NC4=O)CC3)=O)C6=NC=CC=C61
Synonyms

BMS-927711; BHV-3000
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (12)

All Histological Imaging/StainingFlow CytometryIn Vivo Efficacy StudyIFCell Proliferation/Viability Assay

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Journal Impact Factor

Nature

Nociceptive neurons promote gastric tumour progression via a CGRP-RAMP1 axis. [Abstract]

2025 Apr;640(8059):802-810. PMID: 39972142

Rimegepant 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 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.
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

Cancer cells co-opt an inter-organ neuroimmune circuit to escape immune surveillance. [Abstract]

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 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 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).
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 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 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 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.
Br J Pharmacol

Pharmacological characterisation of erenumab, Aimovig, at two CGRP responsive receptors. [Abstract]

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

CGRP reception potentiates anxiety in an influenza A derived immune engram. [Abstract]

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (93.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 4.4 mg/mL (8.23 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8707 mL

9.3535 mL

18.7070 mL

5 mM

0.3741 mL

1.8707 mL

3.7414 mL

10 mM

0.1871 mL

0.9353 mL

1.8707 mL

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (9.35 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (9.35 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (9.35 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

Protocol 5

Add each solvent one by one: 10% EtOH 90% PEG300

Solubility: ≥ 1 mg/mL (1.87 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Nimick M, et al. Pharmacological characterization of ubrogepant and atogepant in cAMP assays at human, rat, and mouse calcitonin family receptors in transfected cells. Biochem Pharmacol. Published online August 30, 2025. [Content Brief]

[2]. Guanglin Luo, 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., 02 Nov 2012.

[3]. Pistolesi A, et al. Biodistribution of atogepant and rimegepant in mouse peripheral and central structures of relevance to migraine pathogenesis. Cephalalgia. 2025;45(11):3331024251378713. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.8707 mL	9.3535 mL	18.7070 mL	46.7674 mL
Ethanol / DMSO	5 mM	0.3741 mL	1.8707 mL	3.7414 mL	9.3535 mL
DMSO	10 mM	0.1871 mL	0.9353 mL	1.8707 mL	4.6767 mL
	15 mM	0.1247 mL	0.6236 mL	1.2471 mL	3.1178 mL
	20 mM	0.0935 mL	0.4677 mL	0.9353 mL	2.3384 mL
	25 mM	0.0748 mL	0.3741 mL	0.7483 mL	1.8707 mL
	30 mM	0.0624 mL	0.3118 mL	0.6236 mL	1.5589 mL
	40 mM	0.0468 mL	0.2338 mL	0.4677 mL	1.1692 mL
	50 mM	0.0374 mL	0.1871 mL	0.3741 mL	0.9353 mL
	60 mM	0.0312 mL	0.1559 mL	0.3118 mL	0.7795 mL
	80 mM	0.0234 mL	0.1169 mL	0.2338 mL	0.5846 mL

Rimegepant

12 Cited Publications

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Rimegepant

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Rimegepant

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rimegepant

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Rimegepant

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rimegepant Related Classifications

HY-15498 Related Classifications