Rimegepant (Synonyms: BMS-927711; BHV-3000)

Name: Rimegepant
Brand: MedChemExpress
SKU: HY-15498
Rating: 5.0 (10 reviews)

Cat. No.: HY-15498 Purity: 99.99%: Data Sheet
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Rimegepant (BMS-927711) 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.

For research use only. We do not sell to patients.

CAS No. : 1289023-67-1

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 10 publication(s) in Google Scholar

Other Forms of Rimegepant:

Rimegepant sulfate hydrate In-stock
Rimegepant hemisulfate Get quote

10 Publications Citing Use of MCE Rimegepant

Histological Imaging/Staining

Flow Cytometry

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

: 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.

: 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.

: 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).

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Biological Activity
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References
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Description

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.

Molecular Weight

534.56

Formula

C₂₈H₂₈F₂N₆O₃

CAS No.

1289023-67-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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, 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.99%

Select Batch:

Data Sheet (288 KB) SDS (393 KB)

COA (263 KB) HNMR (316 KB) RP-HPLC (258 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[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.

[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.

Complete Stock Solution Preparation Table

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 Related Classifications

Neurological Disease

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Rimegepant (Synonyms: BMS-927711; BHV-3000)

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10 Publications Citing Use of MCE Rimegepant

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