IPSU是一种选择性，有口服活性和脑渗透性的OX2R拮抗剂，pKi值为7.85。
| 生物活性 |
IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85. |
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| IC50&Target |
pKi: 7.85 (OX2R), 6.29 (OX1R) |
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| 体外研究 |
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. |
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| 体内研究 |
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 .
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| 分子式 |
C23H27N5O2
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| 分子量 |
405.49
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| CAS号 |
1373765-19-5
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 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。 |
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| 科研文献 |
纯度： 98%
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