WAY-100635 Maleate,99.89%

产品编号:Bellancom-10349A| CAS NO:1092679-51-0| 分子式:C29H38N4O6| 分子量:538.64

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-10349A
900.00 杭州 北京(现货)
Bellancom-10349A
1200.00 杭州 北京(现货)
Bellancom-10349A
4200.00 杭州 北京(现货)
Bellancom-10349A
7200.00 杭州 北京(现货)

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WAY-100635 Maleate

产品介绍 WAY-100635 maleate 是一种有效且具有选择性的 5-hydroxytryptamine 1A (5-HT1A) 受体拮抗剂,其 IC50 值为 0.91 nM,Ki 值为 0.39 nM。WAY-100635 maleate 对于 5-HT1A 和 α1-肾上腺素的 pIC50 值分别为 8.9 和 6.6。WAY-100635 maleate 也是一种有效的多巴胺 D4 受体激动剂。
生物活性

WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist.

体外研究

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D2L or D4.4 receptors.
WAY-100635 displays 940, 370, and 16 nM binding affinities at D2L, D3, and D4.2 receptors, respectively. Saturation analyses demonstrat that the Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D4.4 cells with EC50 of 9.7 nM. WAY-100635 possesses high affinity for D4.4 receptor (3.3 nM) .

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

体内研究

WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat.

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

Animal Model: Male Sprague-Dawley rats (220-240 g)
Dosage: 1 mg/kg
Administration: Subcutaneous injection (Pharmacokinetic study)
Result: Reduced total abstinence score, increased immobility time and the burying behavior was increased.
体内研究

WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat.

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

Animal Model: Male Sprague-Dawley rats (220-240 g)
Dosage: 1 mg/kg
Administration: Subcutaneous injection (Pharmacokinetic study)
Result: Reduced total abstinence score, increased immobility time and the burying behavior was increased.
性状Solid
溶解性数据
In Vitro: 

DMSO : ≥ 250 mg/mL (464.13 mM)

H2O : 25 mg/mL (46.41 mM; Need ultrasonic)

* "≥" 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 1.8565 mL 9.2826 mL 18.5653 mL
5 mM 0.3713 mL 1.8565 mL 3.7131 mL
10 mM 0.1857 mL 0.9283 mL 1.8565 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 (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 25 mg/mL (46.41 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

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