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Rimegepant

🥰Excellent
Catalog No. T4610Cas No. 1289023-67-1
Alias BMS-927711, BMS927711, BMS 927711, 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.

Rimegepant

Rimegepant

🥰Excellent
Purity: 99.84%
Catalog No. T4610Alias BMS-927711, BMS927711, BMS 927711, BHV-3000Cas No. 1289023-67-1
Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.
Pack SizePriceAvailabilityQuantity
1 mg47 €In Stock
5 mg93 €In Stock
10 mg153 €In Stock
25 mg254 €In Stock
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Purity:99.84%
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Product Introduction

Bioactivity
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.
AliasBMS-927711, BMS927711, BMS 927711, BHV-3000
Chemical Properties
Molecular Weight534.56
FormulaC28H28F2N6O3
Cas No.1289023-67-1
SmilesN[C@H]1[C@@H](CC[C@@H](OC(=O)N2CCC(CC2)n2c3cccnc3[nH]c2=O)c2ncccc12)c1cccc(F)c1F
Relative Density.1.45 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (93.53 mM)
Ethanol: <1 mg/mL (insoluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8707 mL9.3535 mL18.7070 mL93.5349 mL
5 mM0.3741 mL1.8707 mL3.7414 mL18.7070 mL
10 mM0.1871 mL0.9353 mL1.8707 mL9.3535 mL
20 mM0.0935 mL0.4677 mL0.9353 mL4.6767 mL
50 mM0.0374 mL0.1871 mL0.3741 mL1.8707 mL

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