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                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。
 HazMat Fee +
 HazMat Fee + 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+ | 
 
                                 
                                
                            

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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。 | |||||||||||||||||||
| 靶点 | 
 | 
| 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]. | 
| 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. | 
| 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 | 
| 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 | |
| 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 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 
 
 
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