Home Tools

Rimegepant

Catalog No. T4610 CAS 1289023-67-1

Synonyms: BMS 927711, BMS-927711, BMS927711, BHV-3000

Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Rimegepant, CAS 1289023-67-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 50.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 162.00
25 mg	In stock	$ 333.00
50 mg	In stock	$ 495.00
100 mg	In stock	$ 719.00
500 mg	In stock	$ 1,490.00
1 mL * 10 mM (in DMSO)	In stock	$ 138.00

Bulk Inquiry

Select Batch

Purity: 99.33%

Purity: 99.16%

Purity: 99.1%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.
Targets&IC50	CGRP receptor:0.14 nM
In vitro	BMS-927711 is a full, competitive CGRP receptor antagonist with IC50 of 0.14±0.01 nM.
In vivo	The mean area under the curve (AUC) (0-24 h) ratios for BMS-927711 at dosages of 60, 100, and 300 mg/kg in the dried blood spot (DBS) matrix versus plasma range from 0.5-0.6 for all doses in rats, indicating a strong correlation between BMS-927711 concentrations in rat plasma and DBS. This study demonstrates that BMS-927711 possesses favorable oral bioavailability in both rats and cynomolgus monkeys, alongside promising preclinical attributes. Furthermore, it exhibits dose-dependent efficacy in a primate model of Calcitonin Gene-Related Peptide (CGRP)-induced facial blood flow, underscoring its potential therapeutic utility.

Synonyms	BMS 927711, BMS-927711, BMS927711, BHV-3000
Molecular Weight	534.56
Formula	C28H28F2N6O3
CAS No.	1289023-67-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL

Ethanol: 10 mg/mL

References and Literature

1. 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) a 2. Zheng N, et al. Improved liquid-liquid extraction with inter-well volume replacement dilution workflow and its application to quantify BMS-927711 in rat dried blood spots by UHPLC-MS/MS. J Pharm Biomed Anal. 2014 Feb;89:240-50.

Citations

1. Sun K, Zhu J, Yan C, et al. CGRP Regulates Nucleus Pulposus Cell Apoptosis and Inflammation via the MAPK/NF-κB Signaling Pathways during Intervertebral Disc Degeneration. Oxidative Medicine and Cellular Longevity. 2021, 2021.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library GPCR Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets

α-CGRP (mouse, rat) TFA CGRP 8-37 (rat) Adrenomedullin (AM) (22-52), human acetate MK-3207 Hydrochloride CGRP antagonist 1 β-CGRP, human acetate Ubrogepant Erenumab

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Rimegepant 1289023-67-1 GPCR/G Protein Neuroscience CGRP Receptor BMS 927711 BHV3000 Inhibitor BMS-927711 BMS927711 Calcitonin gene-related peptide receptor inhibit BHV-3000 BHV 3000 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.