2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. IPSU

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。

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IPSU Chemical Structure

IPSU Chemical Structure

CAS No. : 1373765-19-5

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1210
In-stock
1 mg ￥420
In-stock
5 mg ￥1100
In-stock
10 mg ￥1450
In-stock
25 mg ￥2950
In-stock
50 mg ￥4400
询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

IPSU 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 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].

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

IPSU 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

405.49

Formula

C23H27N5O2
CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 30 mg/mL (73.98 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" 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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Kinase Assay
[2]

Competition experiments are performed with a single concentration of radioligand and six concentrations of competitor (unlabeled ligands; BBAC, almorexant, SB-649868, suvorexant, filorexant or IPSU). 4.6 nM [3H]-BBAC is added simultaneously with various concentrations of unlabeled ligand (0.1 nM-10 μM) to membranes (150 μL/well) in 50 μL/well of assay buffer with a total volume of 250 μL/well. The amount of [3H]-BBAC bound to receptors is determined at room temperature at different time points (ranging from 15 min to 4 h) and terminated by rapid vacuum filtration and liquid scintillation counting[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Freely moving C57Bl/6 mice with chronically implanted electrodes are well abituated to the experiment boxes and had access to food and ater ad libitum. The test compounds (IPSU) or vehicle are administered per os as a suspension in 0.5% methylcellulose immediately prior to lights off and start of recording. Movement is recorded using infrared sensors in the roof of the box. EEG/EMG signals and motility data are used to score 10 s epochs into wake, NREM sleep, and REM sleep. Each animal served as its own control by application and recording of vehicle the day before compound (IPSU) dosing[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

IPSU 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4662 mL 12.3308 mL 24.6615 mL 61.6538 mL
5 mM 0.4932 mL 2.4662 mL 4.9323 mL 12.3308 mL
10 mM 0.2466 mL 1.2331 mL 2.4662 mL 6.1654 mL
15 mM 0.1644 mL 0.8221 mL 1.6441 mL 4.1103 mL
20 mM 0.1233 mL 0.6165 mL 1.2331 mL 3.0827 mL
25 mM 0.0986 mL 0.4932 mL 0.9865 mL 2.4662 mL
30 mM 0.0822 mL 0.4110 mL 0.8221 mL 2.0551 mL
40 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5413 mL
50 mM 0.0493 mL 0.2466 mL 0.4932 mL 1.2331 mL
60 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0276 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IPSU1373765-19-5Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorInhibitorinhibitorinhibit

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