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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.
Alias	BMS-927711, BMS927711, BMS 927711, BHV-3000

Chemical Properties

Molecular Weight	534.56
Formula	C₂₈H₂₈F₂N₆O₃
Cas No.	1289023-67-1
Smiles	N[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

Storage

keep 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), Sonication is recommended.

Ethanol: <1 mg/mL (insoluble)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8707 mL	9.3535 mL	18.7070 mL	93.5349 mL
5 mM	0.3741 mL	1.8707 mL	3.7414 mL	18.7070 mL
10 mM	0.1871 mL	0.9353 mL	1.8707 mL	9.3535 mL
20 mM	0.0935 mL	0.4677 mL	0.9353 mL	4.6767 mL
50 mM	0.0374 mL	0.1871 mL	0.3741 mL	1.8707 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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Tech Support

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