Epelsiban
- CAS No.
- 872599-83-2
- Chemical Name:
- Epelsiban
- Synonyms
- Epelsiban;GSK 557296;(3R,6R)-6-((S)-sec-butyl)-3-(2,3-dihydro-1H-inden-2-yl)-1-((R)-1-(2,6-dimethylpyridin-3-yl)-2-morpholino-2-oxoethyl)piperazine-2,5-dione;(3R,6R)-6-[(2S)-butan-2-yl]-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethylpyridin-3-yl)-2-morpholin-4-yl-2-oxoethyl]piperazine-2,5-dione;2,5-Piperazinedione, 3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-, (3R,6R)-
- CBNumber:
- CB63126529
- Molecular Formula:
- C30H38N4O4
- Molecular Weight:
- 518.65
- MDL Number:
- MFCD26961099
- MOL File:
- 872599-83-2.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Boiling point | 790.6±60.0 °C(Predicted) |
|---|---|
| Density | 1.214±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | Soluble in DMSO |
| pka | 13.16±0.60(Predicted) |
| FDA UNII | T2EZ19HX73 |
Epelsiban price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biosynth | XJB59983 | Epelsiban | 872599-83-2 | 5mg | $1670.55 | 2026-06-05 | Buy |
| Biosynth | XJB59983 | Epelsiban | 872599-83-2 | 10mg | $2672.8 | 2026-06-05 | Buy |
| Biosynth | XJB59983 | Epelsiban | 872599-83-2 | 25mg | $5011.5 | 2026-06-05 | Buy |
| Biosynth | XJB59983 | Epelsiban | 872599-83-2 | 50mg | $8018.5 | 2026-06-05 | Buy |
Epelsiban Chemical Properties, Uses, Production
Uses
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
Definition
ChEBI: Epelsiban is a dipeptide.
in vivo
Epelsiban shows an IC50 of 192 nM for oxytocin receptor in rats. Epelsiban has low levels of intrinsic clearance against the microsomes of rat, dog, and cynomolgus monkey, good bioavailability (55%), but is negative in the genotoxicity screens with a satisfactory oral safety profile in female rats[1].
References
[1] Borthwick AD, et al. Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency. J Med Chem. 2012 Jan 26;55(2):783-96. DOI:10.1021/jm201287w
Epelsiban Preparation Products And Raw materials
Raw materials
Preparation Products
Epelsiban Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9718 | 58 |
| Shanghai zhigan biotechnology co., LTD | zhiqianbio@126.com | China | 19765 | 58 | |
| BOC Sciences | 16314854226; +8616314854226 | inquiry@bocsci.com | United States | 19852 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| Shandong Ziyi Pharmaceutical Co., Ltd. | 17860786593 | 1181917242@qq.com | China | 9999 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 38999 | 58 |
