Name: BMS-927711 (Rimegepant)
Brand: Selleck Chemicals
SKU: S6659
Availability: InStock
Rating: 5 (1 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other CGRP Receptor Inhibitors	Atogepant Vazegepant hydrochloride Ubrogepant Olcegepant Rat CGRP-(8-37)

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (187.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	534.56	Formula	C₂₈H₂₈F₂N₆O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1289023-67-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BHV-3000			Smiles	C1CC(C2=C(C=CC=N2)C(C1C3=C(C(=CC=C3)F)F)N)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6

Mechanism of Action

Targets/IC₅₀/Ki	CGRP receptor (Cell-free assay) 0.027 nM(Ki)
In vitro	Rimegepant (BMS-927711, BHV-3000) is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist with ki of 0.027 nM.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23153230/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06409832	Recruiting	Migraine\|Migraine With Aura\|Migraine Without Aura\|Chronic Migraine	University of Florence\|IRCCS National Neurological Institute C. Mondino Foundation\|Società italiana per lo studio delle Cefalee (SISC)\|Azienda Ospedaliero-Universitaria Consorziale Policlinico di Bari\|Università degli Studi dell''Aquila\|University of Roma La Sapienza\|Azienda Ospedaliero Universitaria Policlinico Modena\|Ospedale di Piove di Sacco\|Azienda Ospedaliero-Universitaria di Parma\|Azienda Ospedaliera S. Maria della Misericordia\|Azienda Ospedaliera Città della Salute e della Scienza di Torino\|Cliniche Humanitas Gavazzeni\|University of Campania Luigi Vanvitelli\|Ospedale di Prato\|Azienda Policlinico Umberto I\|Auxologico San Luca Milano\|ASST Spedali Civili Brescia\|Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta	March 26 2024	--
NCT05888766	Not yet recruiting	Migraine Disorders	University of Roma La Sapienza	July 1 2023	--
NCT05518123	Recruiting	Migraine	Pfizer	November 7 2022	Phase 4
NCT05509400	Recruiting	Migraine	Pfizer	October 18 2022	Phase 4
NCT05399485	Active not recruiting	Migraine	Pfizer	August 9 2022	Phase 3
NCT05262517	Terminated	Temporomandibular Disorders (TMD)	Pfizer	May 5 2022	Phase 3

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BMS-927711 (Rimegepant) CGRP Receptor antagonist

Chemical Structure

Molecular Weight: 534.56