IPSU,98.10%

产品编号:Bellancom-13796| CAS NO:1373765-19-5| 分子式:C23H27N5O2| 分子量:405.49

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-13796
1400.00 杭州 北京(现货)
Bellancom-13796
1800.00 杭州 北京(现货)
Bellancom-13796
3800.00 杭州 北京(现货)
Bellancom-13796
6800.00 杭州 北京(现货)

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IPSU

产品介绍 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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状Solid
溶解性数据
In Vitro: 

DMSO : ≥ 30 mg/mL (73.98 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4662 mL 12.3308 mL 24.6615 mL
5 mM 0.4932 mL 2.4662 mL 4.9323 mL
10 mM 0.2466 mL 1.2331 mL 2.4662 mL
*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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