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Tranylcypromine (2-PCPA) hydrochloride

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产品编号 T1025Cas号 1986-47-6
别名 反苯环丙胺盐酸盐, Tranylcypromine (2-PCPA) HCl, SKF-385 HCl

Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl) 是一种单胺氧化酶抑制剂,对治疗重度抑郁症、心境恶劣障碍和非典型抑郁症有效。

Tranylcypromine (2-PCPA) hydrochloride

Tranylcypromine (2-PCPA) hydrochloride

Rating icon 很棒
纯度: 99.86%
产品编号 T1025 别名 反苯环丙胺盐酸盐, Tranylcypromine (2-PCPA) HCl, SKF-385 HClCas号 1986-47-6

Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl) 是一种单胺氧化酶抑制剂,对治疗重度抑郁症、心境恶劣障碍和非典型抑郁症有效。

规格价格库存数量
50 mg
¥ 258
现货
100 mg
¥ 413
现货
200 mg
¥ 543
现货
500 mg
¥ 849
现货
1 mL x 10 mM (in DMSO)
¥ 150
现货
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纯度:99.86%
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产品介绍

生物活性
产品描述
Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl), a Monoamine Oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression.
靶点活性
MAO-B:7 μM, MAO-A:11.5 μM, LSD1:22.3 μM
体外活性
与空白对照组相比,Tranylcypromine(5 mg/kg和10 mg/kg)可大而缓的增加雄性大鼠的肌肉活动,但2 mg/kg的Tranylcypromine没有效果. Tranylcypromine(10 mg/kg)使雄性大鼠饲养行为数量显著增加.
体内活性
在小牛主动脉内皮细胞中,Tranylcypromine(500 μg/mL)可强烈抑制缓激肽诱导的花生四烯酸释放。 Tranylcypromine还能抑制HLMs中的CYP2A6(IC50:0.42 μM)和CYP2E1(IC50:3 μM)活性。在HLMs中,Tranylcypromine引起II型和环丙基苯I型的差异谱。HLMs中CYP2A6介导的尼古丁代谢可被R-(+)-Tranylcypromine(Ki:0.05 μM),(±)-Tranylcypromine(Ki:0.08 μM)以及S-(-)-Tranylcypromine(Ki:2.0 μM)完全抑制。
激酶实验
PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl2, 0.5 μM cAMP or cGMP, and [3H]cAMP or [3H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration[3].
别名反苯环丙胺盐酸盐, Tranylcypromine (2-PCPA) HCl, SKF-385 HCl
化学信息
分子量169.66
分子式C9H11N·HCl
CAS No.1986-47-6
SmilesN[C@H]1[C@H](C2=CC=CC=C2)C1.Cl
密度no data available
储存&溶解度
存储store under nitrogen,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: 17 mg/mL (100.2 mM), Sonication is recommended.
DMSO: 65 mg/mL (383.12 mM), Sonication is recommended.
溶液配制表
H2O/DMSO
1mg5mg10mg50mg
1 mM5.8941 mL29.4707 mL58.9414 mL294.7071 mL
5 mM1.1788 mL5.8941 mL11.7883 mL58.9414 mL
10 mM0.5894 mL2.9471 mL5.8941 mL29.4707 mL
20 mM0.2947 mL1.4735 mL2.9471 mL14.7354 mL
50 mM0.1179 mL0.5894 mL1.1788 mL5.8941 mL
100 mM0.0589 mL0.2947 mL0.5894 mL2.9471 mL

SCI 文献

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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