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Rimegepant

SKU: orb1302712

Description

Rimegepant

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number1289023-67-1
MW534.56
Purity99.99%
FormulaC28H28F2N6O3
SMILESN[C@H]1[C@@H](CC[C@@H](OC(=O)N2CCC(CC2)n2c3cccnc3[nH]c2=O)c2ncccc12)c1cccc(F)c1F
TargetCGRP Receptor
SolubilityDMSO:70 mg/mL (130.95 mM);Ethanol:< 1 mg/mL (insoluble)

Bioactivity

Target IC50
CGRP receptor:0.14 nM|CGRP receptor:0.027 nM (Ki)
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.
In Vitro
BMS-927711 is a full, competitive CGRP receptor antagonist with IC50 of 0.14±0.01 nM.

Storage & Handling

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/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

BMS927711, BMS-927711, BMS 927711, BHV 3000, BHV3000, BHV-3000, Calcitonin gene-related peptide receptor, CGRPReceptor, CGRP Receptor, CGRP, Inhibitor, inhibit, Rimegepant

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Quality Guarantee

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Key Properties

No computed properties available.

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Rimegepant (orb1302712)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 90.00
5 mg
$ 140.00
1 ml x 10 mM (in DMSO)
$ 160.00
10 mg
$ 200.00
25 mg
$ 300.00
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