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IPSU
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IPSU图片
CAS NO:1373765-19-5
包装与价格:
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

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 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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM2.4662 mL12.3308 mL24.6615 mL
5 mM0.4932 mL2.4662 mL4.9323 mL
10 mM0.2466 mL1.2331 mL2.4662 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。