| CAS NO: | 872599-83-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Name: Epelsiban CAS#: 872599-83-2 Chemical Formula: C30H38N4O4 Exact Mass: 518.2893 Molecular Weight: 518.658 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: GSK-557296; GSK 557296; GSK557296; GSK-557,296-B Chemical Name: (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 InChi Key: UWHCWRQFNKUYCG-QUZACWSFSA-N InChi Code: InChI=1S/C30H38N4O4/c1-5-18(2)26-28(35)32-25(23-16-21-8-6-7-9-22(21)17-23)29(36)34(26)27(24-11-10-19(3)31-20(24)4)30(37)33-12-14-38-15-13-33/h6-11,18,23,25-27H,5,12-17H2,1-4H3,(H,32,35)/t18-,25+,26+,27+/m0/s1 SMILES Code: O=C([C@@H](C1CC2=C(C=CC=C2)C1)N3)N([C@H](C4=CC=C(C)N=C4C)C(N5CCOCC5)=O)[C@H]([C@@H](C)CC)C3=O |
| In Vitro | Epelsiban (GSK557296; GSK-557296) 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), and shows no significant P450 inhibition[1]. |
|---|---|
| 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]. |
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