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WAY-100635
5-HT1A受体拮抗剂,WAY-100635是5-HT受体拮抗剂,IC50为0.95nM。
目录号: PC14102 纯度: ≥98%
CAS No. :162760-96-5
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中文名称
WAY-100635
中文别名
N-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-N-2-吡啶基-环己烷羧胺
英文名称
WAY-100635
英文别名
CYCLOHEXANECARBOXAMIDE, N-[2-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL]ETHYL]-N-2-PYRIDINYL-, HYDROCHLORIDE (1:3);Cyclohexanecarboxamide, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-;N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide;WAY-100635;WAY100635 TRIHYDROCHLORIDE;WAY 100635;N-{2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxaMide;CYCLOHEXANECARBOXYLIC ACID (2-[4-(2-METHOXY-PHENYL)-PIPERAZIN-1-YL]-ETHYL)-PYRIDIN-2-YL-AMIDE TRIHYDROCHLORIDE
Cas No.
162760-96-5
分子式
C25H34N4O2
分子量
422.56
包装储存
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 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 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.

性状

Oil

IC50 & Target[1][2]

5-HT1A Receptor

8.87 (pIC50)

5-HT1A Receptor

9.71 (pA2)

体外研究(In Vitro)

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 [H] 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) .

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

体内研究(In Vivo)

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.

Medlife 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.
运输条件

Room temperature or refrigerated transportation.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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