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Rimegepant

Catalog No. T4610 CAS 1289023-67-1

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

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

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Rimegepant, CAS 1289023-67-1

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	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 ratios of the mean AUC (0-24 h) values for 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 BMS-927711 concentrations between rat plasma and rat blood (DBS).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

Synonyms	BMS 927711, BMS927711, BHV-3000, BMS-927711
Molecular Weight	534.568
Formula	C28H28F2N6O3
CAS No.	1289023-67-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 10 mg/mL

Ethanol: 10 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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：

GPCR Compound Library Endocrinology-Hormone Compound Library Inhibitor Library Ion Channel Inhibitor Library Drug Repurposing Compound Library FDA-Approved Drug Library Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

β-CGRP, human acetate Adrenomedullin (AM) (22-52), human acetate HCGRP-(8-37) acetate Calcitonin（salmon） Acetate(47931-85-1(free base)) Calcitonin (salmon) Vazegepant hydrochloride MK-3207 Hydrochloride Rimegepant

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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 离子通道 CGRP Receptor Inhibitor BMS 927711 Calcitonin gene-related peptide receptor BMS-927711 inhibit BHV-3000 BMS927711 inhibitor

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