1. GPCR/G Protein
    Neuronal Signaling
  2. CGRP Receptor
  3. Rimegepant

Rimegepant (Synonyms: BMS-927711)

Cat. No.: HY-15498 Purity: 99.08%
Handling Instructions

Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.

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

Rimegepant Chemical Structure

Rimegepant Chemical Structure

CAS No. : 1289023-67-1

Size Price Stock Quantity
5 mg USD 140 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor[1].

IC50 & Target

Ki: 0.027 nM (CGRP receptor)[1]
IC50: 0.14 nM (CGRP receptor)[1]

In Vitro

Rimegepant (BMS-927711) is a full, competitive CGRP receptor antagonist with IC50 of 0.14±0.01 nM[1].

In Vivo

Rimegepant (BMS-927711) has good oral bioavailability in rat and cynomolgus monkey, attractive overall preclinical properties, and shows dose-dependent activity in a primate model of CGRP-induced facial blood flow[1]. The ratios of the mean AUC (0-24 h) values for Rimegepant (BMS-927711) (60, 100, and 300 mg/kg) in the DBS matrix, compare with plasma, are 0.5-0.6 across all doses in rats. Results from this study suggest a strong correlation of Rimegepant concentrations between rat plasma and rat blood (DBS)[2].

Clinical Trial
Molecular Weight

534.56

Formula

C₂₈H₂₈F₂N₆O₃

CAS No.

1289023-67-1

SMILES

N[[email protected]]1[[email protected]](C2=C(F)C(F)=CC=C2)CC[[email protected]@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

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (18.71 mM; Need ultrasonic and warming)

Ethanol : 10 mg/mL (18.71 mM; Need ultrasonic and warming)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

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

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Rats[2]
Rats are treated with drug-free vehicle (control) or Rimegepant (BMS-927711) in vehicle at 60, 100, and 300 mg/kg once daily via oral gavage. There are 6 rats in each treatment group. For each treatment group, blood is collected at 1, 6, and 24 h from first three rats, and at 3 and 8 h from the second three rats on Day 1 and Day 14 from the tail vein following daily oral dosing of Rimegepant (BMS-927711) for two weeks. The mean hematocrits in the blood are 50.2±1.8%, 49.8±2.2%, 46.4±5.2% corresponding to the animal groups of 60, 100, and 300 mg/kg doses, respectively. For DBS evaluation, four 15 μL blood samples are spotted onto DBS cards (4 spots per card), dried at room temperature for at least 2 h, and each card is packaged separately in a ziplock bag with desiccant prior to shipment. The remaining blood in each sample tube is processed to plasma within 1 h of collection and stored at -70°C until analysis. Plasma samples are shipped on dry ice, and DBS cards are shipped at ambient temperature. Rimegepant (BMS-927711) concentrations in rat plasma are analyzed. Rimegepant in rat DBS is analyzed using the DBS method. The toxicokinetic (TK) parameters are calculated from blood concentration and time data using non-compartmental methods using Kinetica.

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

References

Purity: 99.08%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

RimegepantBMS-927711BMS927711BMS 927711CGRP ReceptorCalcitonin gene-related peptide receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
Rimegepant
Cat. No.:
HY-15498
Quantity:
MCE Japan Authorized Agent: