IPSU - CAS:1373765-19-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	IPSU
英文名称:	IPSU
别名:	IPSU 2-(1H-Indol-3-ylmethyl)-9-(4-methoxy-2-pyrimidinyl)-2,9-diazaspiro[5.5]undecan-1-one
CAS No:	1373765-19-5	分子式:	C₂₃H₂₇N₅O₂	分子量:	405.49
CAS No:	1373765-19-5
分子式:	C₂₃H₂₇N₅O₂
分子量:	405.49

点击下载产品说明书(PDF)

I10480 IPSU ≥98% (psaitong)

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包装规格：

5mg 10mg 25mg 50mg in glass bottle

溶解性：

溶于DMSO(≥30mg/mL）

产品描述：

基本信息

产品编号：	I10480
产品名称：	IPSU
CAS:	1373765-19-5	储存条件	粉末	-20℃	四年

分子式：	C23H27N5O2		溶于液体	-80℃	6个月
分子量：	405.49			-20℃	1个月
化学名：	2-(1H-Indol-3-ylmethyl)-9-(4-methoxy-2-pyrimidinyl)-2,9-diazaspiro[5.5]undecan-1-one
Solubility (25°C)：
体外:	DMSO	31mg/mL (69.2mM)
	Ethanol	Insoluble
	Water	Insoluble
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.4662mL	12.3308mL	24.6615mL
5mM	0.4932mL	2.4662mL	4.9323mL
10mM	0.2466mL	1.2331mL	2.4662mL

生物活性

产品描述	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。
靶点	pKi:7.85 (OX2R),6.29 (OX1R)
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.
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 4-5h,after which time the total sleep time per hour is the same as on vehicle day .

推荐实验方法(仅供参考)

激酶实验：

ligands;BBAC,almorexant,SB-649868,suvorexant,filorexant or IPSU).4.6nM [3H]-BBAC is added simultaneously with various concentrations of unlabeled ligand (0.1nM-10μM) to membranes (150μL/well) in 50μL/well of assay buffer with a total volume of 250μL/well.The amount of [3H]-BBAC bound to receptors is determined at room temperature at different time points (ranging from 15 min to 4h) and terminated by rapid vacuum filtration and liquid scintillation counting.

细胞实验:
细胞系	人脐静脉内皮细胞(HUVECs)
浓度	0.01,0.1,1μM
处理时间	10 min
方法	用不同浓度的JTE-013对HUVECs进行预处理，处理10分钟，然后让HUVECs向下层小室迁移4h（下层小室中具有特定浓度的Sph-1-P）。收集、固定迁移过来的、在滤网下层的细胞，并进行染色和计数。