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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $46 | In Stock | In Stock | |
| 5 mg | $88 | In Stock | In Stock | |
| 10 mg | $145 | In Stock | In Stock | |
| 25 mg | $242 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $113 | In Stock | In Stock |
| 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, CGRP receptor:0.027 nM (Ki) |
| 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. |
| Synonyms | BMS-927711, BMS927711, BMS 927711, BHV-3000 |
| 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 | keep away from direct sunlight,keep away from moisture,store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 70 mg/mL (130.95 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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