CAS NO: | 872599-83-2 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | Epelsiban (GSK 557296) is a potent, selective and orally bioavailableoxytocin receptorantagonist, with apKiof 9.9 for humanoxytocin receptor. |
IC50& Target | pKi: 9.9 (human oxytocin receptor)[1] |
体外研究 (In Vitro) | Epelsiban is a potent oxytocin receptor, with a pKiof 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]. |
体内研究 (In Vivo) | Epelsiban shows an IC50of 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]. |
Clinical Trial | |
分子量 | 518.65 |
Formula | C30H38N4O4 |
CAS 号 | 872599-83-2 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |