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Epelsiban
Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).
Catalog No. T11502Cas No. 872599-83-2
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Epelsiban
Catalog No. T11502Cas No. 872599-83-2
Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $2,120 | 8-10 weeks | |
| 50 mg | $2,780 | 8-10 weeks | |
| 100 mg | $3,700 | 8-10 weeks |
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Chemical Properties
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| Description | Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor). |
| Targets&IC50 | OTR (human):(pKi)9.9 , OTR (human):192 nM |
| In vitro | Epelsiban , shows no significant P450 inhibition.?is a potent oxytocin receptor, with a pKi of 9.9 for human oxytocin receptor, >31000-fold selectivity over all three human vasopressin receptors hV1aR (pKi, <5.2), hV2R (pKi, <5.1), and hV1bR (pKi, 5.4). |
| In vivo | Epelsiban exhibits low intrinsic clearance in rat, dog, and cynomolgus monkey microsomes, demonstrating good bioavailability (55%) while showing no genotoxic effects, and maintaining a satisfactory safety profile when orally administered to female rats. Additionally, Epelsiban effectively inhibits the oxytocin receptor in rats with an IC50 of 192 nM. |
| Alias | GSK 557296 |
| Molecular Weight | 518.65 |
| Formula | C30H38N4O4 |
| Cas No. | 872599-83-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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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 . A total of 10 animals were administered, and the formula you used is 5% 
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 (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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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
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