IPSU

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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。

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，pK_i值为7.85。

生物活性

IPSU is a selective, orally available and brain penetrantOX2Rantagonist with apK_iof 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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 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℃, 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。