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Tranylcypromine HCl {[allProObj[0].p_purity_real_show]}

货号:A116070 同义名: 反式-2-苯基环丙胺 / SKF 385 hydrochloride; Tranylcypromine (hydrochloride)

Tranylcypromine hydrochloride是一种双重MAO-A/B和LSD1抑制剂。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Tranylcypromine HCl 化学结构 CAS号:1986-47-6
Tranylcypromine HCl 化学结构
CAS号:1986-47-6
Tranylcypromine HCl 3D分子结构
CAS号:1986-47-6
Tranylcypromine HCl 化学结构 CAS号:1986-47-6
Tranylcypromine HCl 3D分子结构 CAS号:1986-47-6
规格 价格 会员价 库存 数量
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Tranylcypromine HCl 纯度/质量文件 产品仅供科研

货号:A116070 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 MAO MAO-A MAO-B 其他靶点 纯度
Sennoside A ++

MAO, IC50: 17 μM

98%+
Glycyrrhizic acid ++++

MAO, IC50: 0.16 μM

80% HPLC
Rasagiline ++++

MAO-A, IC50: 412 nM

++++

MAO-B, IC50: 4.43 nM

97%
Isatin ++

MAO, IC50: 15 μM

+

MAO-A, IC50: 58 μM

++

MAO-B, IC50: 14 μM

98%
Paeonol +

MAO-A, IC50: 54.6 μM

+

MAO-B, IC50: 42.5 μM

98%
Tranylcypromine HCl +++

MAO-A, IC50: 11.5 μM

+++

MAO-B, IC50: 7 μM

97%
Moclobemide +++

MAO-A (5-HT), IC50: 6.1 μM

99%+
Pargyline HCl ++

MAO-A, Ki: 13 μM

+++

MAO-B, Ki: 0.5 μM

99%+
Safinamide ++++

MAO-B, IC50: 98 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Tranylcypromine HCl 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].

Tranylcypromine HCl 细胞实验

Cell Line
Concentration Treated Time Description References
NCI-H510A 0.002 to 2000 nM 10 days Evaluate the effect of Tranylcypromine on SCLC cell viability ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834.
Jurkat cells 10 µM 12 hours Evaluate the effect on LSD1-dependent transcriptional regulation, results showed S1427 significantly downregulated NOTCH3 expression ACS Med Chem Lett. 2022 Apr 29;13(5):848-854.
MV(4;11) 0.002 to 2000 nM 24 hours Evaluate the effect of Tranylcypromine on LSD1 target engagement ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834.
Human prostate carcinoma (LNCaP-LN3) cells 0.5, 1, 1.5, 2 mM 24, 48, 72, 96, 120 hours To investigate the effect of Tranylcypromine on cell proliferation, results showed increased proliferation in Tranylcypromine-treated cells Oncol Rep. 2013 Oct;30(4):1587-92.
Human lung epithelial cells (A549) 0.5 and 1 mM 48 hours To evaluate the antiviral effect of TCP on HSV-1 and adenovirus, results showed that TCP at 1 mM significantly reduced viral titers. Antimicrob Agents Chemother. 2014 May;58(5):2807-15.
Mouse neuronal cells (N18) 0.5 and 1 mM 48 hours To evaluate the antiviral effect of TCP on HSV-1, results showed that TCP at 1 mM significantly reduced HSV-1 titers. Antimicrob Agents Chemother. 2014 May;58(5):2807-15.
Primary astrocytes 5 µM 5.5 hours Tranylcypromine did not alter LPS-induced proinflammatory cytokine levels Cells. 2020 Aug 28;9(9):1982.
BV2 microglial cells 5 µM 5.5 hours Tranylcypromine significantly decreased LPS-induced IL-1β and IL-6 mRNA levels Cells. 2020 Aug 28;9(9):1982.
THP-1 0.002 to 2000 nM 96 hours Evaluate the effect of Tranylcypromine on CD11b marker induction ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834.
TF-1a 0.002 to 2000 nM 96 hours Evaluate the effect of Tranylcypromine on AML cell viability ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834.

Tranylcypromine HCl 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Induced endometriosis model Intra-peritoneal injection 1 or 2 mg/kg Every two days for two weeks Significantly and substantially reduced the lesion size and improved generalized hyperalgesia in a dose-dependent fashion Reprod Biol Endocrinol. 2016 Apr 9;14:17
ICR mice Xenoplanted mouse cancer model Intraperitoneal injection 10 mg/5 mL/kg Single dose Evaluate pharmacokinetic profiles, results showed S1427 had significantly better AUC0?∞, Cmax, and T1/2 compared to S2157 ACS Med Chem Lett. 2022 Apr 29;13(5):848-854.
ICR mice HSV-1 infection model Topical on cornea and intraperitoneal injection 10 mg/kg Once daily for 3 days To evaluate the in vivo antiviral effect of TCP on HSV-1 infection, results showed that TCP pretreatment significantly reduced viral titers in mouse eyes. Antimicrob Agents Chemother. 2014 May;58(5):2807-15.
Male C57BL/6J mice Noise-induced permanent threshold shift hearing loss model Intraperitoneal injection 2 mg/kg Daily for 2 weeks Tranylcypromine upregulated Sestrin 2 expression, activated autophagy markers LC3B and LAMP1, reduced levels of 4-HNE and cleaved caspase-3, thereby mitigating noise-induced hair cell loss and hearing impairment. Neural Regen Res. 2025 May 1;20(5):1483-1494
Wild-type mice LPS-induced neuroinflammation model Intraperitoneal injection 3 mg/kg Daily for 3 days Tranylcypromine significantly reduced LPS-induced microglial activation and proinflammatory cytokine COX-2 and IL-6 levels Cells. 2020 Aug 28;9(9):1982.
Rats Nicotine self-administration model Intraperitoneal injection 3 mg/kg 1-hour or 20-hour pretreatment To study the mechanisms by which tranylcypromine enhances nicotine self-administration independent of MAO inhibition Neuropharmacology. 2011 Jul-Aug;61(1-2):95-104

Tranylcypromine HCl 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

Tranylcypromine HCl 实验方案

计算器
存储液制备 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

Tranylcypromine HCl 技术信息

CAS号1986-47-6
分子式C9H12ClN
分子量 169.65
SMILES Code N[C@H]1[C@H](C2=CC=CC=C2)C1.[H]Cl
MDL No. MFCD00063602
别名 反式-2-苯基环丙胺 ;SKF 385 hydrochloride; Tranylcypromine (hydrochloride); trans-2-Phenylcyclopropylamine; 2-PCPA; Tranylcypromine HCl
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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