| 名称 | Tranylcypromine (2-PCPA) hydrochloride |
| 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. |
| 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]. |
| 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。 |
| 存储条件 | Store under nitrogen,Store at low temperature,Keep away from moisture,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : 100 mg/mL (589.41 mM), Sonication is recommended.
DMSO : 250 mg/mL (1473.54 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (11.79 mM), Sonication is recommended.
10% DMSO+90% Saline : 10 mg/mL (58.94 mM), Solution.
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| 关键字 | Tranylcypromine (2-PCPA) Hydrochloride | Tranylcypromine (2PCPA) hydrochloride | Tranylcypromine (2 PCPA) hydrochloride | MAO | LSD1 | HistoneDemethylase | Histone Demethylase |
| 相关产品 | β-Aminopropionitrile | Safinamide | 1,4-Naphthoquinone | Procaine | Hydroxylamine hydrochloride | 4-Chlorochalcone | Methylene Blue trihydrate | Eicosapentaenoic Acid | D-(-)-Quinic acid | Allylthiourea | Aminoacetone hydrochloride | Paeonol |
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