Tranylcypromine HCl

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Chemical Structure| 1986-47-6 同义名 : 反式-2-苯基环丙胺 ;SKF 385 hydrochloride; Tranylcypromine (hydrochloride); trans-2-Phenylcyclopropylamine; 2-PCPA; Tranylcypromine HCl
CAS号 : 1986-47-6
货号 : A116070
分子式 : C9H12ClN
纯度 : 97%
分子量 : 169.65
MDL号 : MFCD00063602
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(618.92 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(589.44 mM)，配合低频超声助溶
生物活性
靶点

  • MAO-B

    MAO-B, IC50:7 μM

  • MAO-A

    MAO-A, IC50:11.5 μM
描述 Trans-2-Phenylcyclopropylamine (2-PCPA) is a time-dependent, mechanism-based irreversible inhibitor of LSD1 with a KI of 242 mM and a kinact of 0.0106 s-1. 2-PCPA shows limited selectivity for human MAOs versus LSD1, with kinact/KI values only 16-fold and 2.4-fold higher for MAO B and MAO A, respectively[3]. 2-PCPA-based inhibitors featuring substitutions on the amino group have emerged, with sub-micromolar affinities toward LSD1 (Lysine-specific demethylase 1) and high selectivities over monoamine oxidases (MAOs)[4]. Mice treated with the antidepressant trans-2-phenylcyclopropylamine (2-PCPA) were protected against diet-induced-obesity, and adiposity was reversed in pre-established diet-induced obese mice. 2-PCPA can reduce obesity by decreasing food intake in the long term while increasing activity in the short-term[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.89mL

1.18mL

0.59mL

29.47mL

5.89mL

2.95mL

58.94mL

11.79mL

5.89mL
参考文献

[1]Zhang W, Kilicarslan T, et al. Evaluation of methoxsalen, tranylcypromine, and tryptamine as specific and selective CYP2A6 inhibitors in vitro. Drug Metab Dispos. 2001 Jun;29(6):897-902.

[2]Hong SL, Carty T, Deykin D. Tranylcypromine and 15-hydroperoxyarachidonate affect arachidonic acid release in addition to inhibition of prostacyclin synthesis in calf aortic endothelial cells. J Biol Chem. 1980 Oct 25;255(20):9538-40.

[3]Schmidt DM, McCafferty DG. trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1. Biochemistry. 2007 Apr 10;46(14):4408-16

[4]Niwa H, Sato S, Handa N, Sengoku T, Umehara T, Yokoyama S. Development and Structural Evaluation of N-Alkylated trans-2-Phenylcyclopropylamine-Based LSD1 Inhibitors. ChemMedChem. 2020 May 6;15(9):787-793

[5]Shemesh A, Abdulla A, Yang F, Chua SC, Pessin JE, Zong H. The antidepressant trans-2-phenylcyclopropylamine protects mice from high-fat-diet-induced obesity. PLoS One. 2014 Feb 21;9(2):e89199