CAS NO: | 1373765-19-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | IPSU is a selective, orally available and brain penetrantOX2Rantagonist with apKiof 7.85. | ||||||||||||||||
IC50& Target | pKi: 7.85 (OX2R), 6.29 (OX1R)[1] | ||||||||||||||||
体外研究 (In Vitro) | Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays[2]. | ||||||||||||||||
体内研究 (In Vivo) | IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day[1]. | ||||||||||||||||
分子量 | 405.49 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H27N5O2 | ||||||||||||||||
CAS 号 | 1373765-19-5 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 30 mg/mL(73.98 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |