反苯环丙胺盐酸盐 T1025

Product Introduction
Bioactivity


英文名: Tranylcypromine (2-PCPA) hydrochloride

描述: 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。

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: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 17 mg/mL (100 mM)
DMSO : 17 mg/mL (100 mM)


关键字: Tranylcypromine (2-PCPA) Hydrochloride | Tranylcypromine (2PCPA) hydrochloride | Tranylcypromine (2 PCPA) hydrochloride

相关产品: NCGC00244536 | KDM5-IN-1 | KDM5-C70 | Daminozide | S2101 | CPI-455 HCl | JQKD82 trihydrochloride | Ryuvidine | SD49-7 | KDM5A-IN-1

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Lipid Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Highly Selective Inhibitor Library | Anti-Cardiovascular Disease Compound Library

反苯环丙胺盐酸盐 T1025信息由TargetMol中国为您提供，如您想了解更多关于反苯环丙胺盐酸盐 T1025报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途