Free shipping on all orders over $ 500

Rimegepant

Cat. No. M9165
Rimegepant Structure
Synonym:

BMS-927711; BHV-3000

Size Price Availability Quantity
2mg USD 80  USD80 In stock
5mg USD 150  USD150 In stock
10mg USD 240  USD240 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

Rimegepant, also known as BMS-927711, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist with a Ki value of 0.027 nM. Rimegepant has shown in vivo efficacy without vasoconstriction effect. BMS-927711 is superior to placebo at several different doses (75 mg, 150 mg, and 300 mg) and has an excellent tolerability profile. The compound is unstable in solutions, freshly prepared is recommended.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 534.56
Formula C28H28F2N6O3
CAS Number 1289023-67-1
Purity 98.17%
Solubility DMSO 9 mg/mL
Ethanol 9 mg/mL
Storage Powder
References

[1] Zheng N, et al. J Pharm Biomed Anal. 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.

[2] Zheng N, et al. J Pharm Biomed Anal. A rapid, accurate and robust UHPLC-MS/MS method for quantitative determination of BMS-927711, a CGRP receptor antagonist, in plasma in support of non-clinical toxicokinetic studies.

Related CGRP Receptor Products
Ubrogepant

Ubrogepant (MK-1602) is a novel oral calcitonin gene-associated peptide receptor (CGRP) antagonist with the potential to be used in acute migraine studies.

Calcitonin (salmon)

Calcitonin salmon is a calcium-regulating hormone that is a dual agonist of amylin and calcitonin receptors that stimulate bone production and inhibit bone resorption.

Vazegepant hydrochloride

Vazegepant (BHV-3500) hydrochloride is a highly affinity CGRP receptor antagonist (hCGRP Ki= 0.023 nM).

Olcegepant (BIBN-4096)

Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide (CGRP) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.

BAR501

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

  Catalog
Abmole Inhibitor Catalog




Keywords: Rimegepant, BMS-927711; BHV-3000 supplier, CGRP Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.