Clorgyline HCl

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Chemical Structure| 17780-75-5 同义名 : N-2,4-Dichlorophenoxypropyl-N-methylpropargylamine;Clorgyline (hydrochloride);Clorgyline hydrochloride
CAS号 : 17780-75-5
货号 : A101686
分子式 : C13H16Cl3NO
纯度 : 99%+
分子量 : 308.631
MDL号 : MFCD00052012
存储条件:

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(340.21 mM),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(324.01 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Clorgiline Hydrochloride is an irreversible and selective MAO-A inhibitor with IC50 of 6.061 ± 0.262 µM[3]. MAO A inhibitors reduce the growth of prostate cancer, drug sensitive and resistant gliomas and classical Hodgkin lymphoma, and enhance standard chemotherapy[4]. The MAOA inhibitor clorgyline reduced the growth of L1236 cells and U-HO1 cells, and shRNA knockdown of MAOA reduced the growth of L1236 cells. Combined treatment with clorgyline and ABVD (doxorubicin, bleomycin, vinblastine, dacarbazine) was more effective in reducing cell growth than either regimen alone[5]. In human SH-SY5Y cells expressing MAO-A but not MAO-B, hypoxia significantly increased the MAO-A expression, which was blocked by M30 or clorgyline[6]. Clorgyline, induced secretory differentiation in primary cultures of normal basal epithelial cells and high-grade PCa (primary prostate cancer). Treatment with clorgyline in vitro inhibited growth and altered the transcriptional pattern of VCaP cells in a manner consistent with the pro-differentiation and anti-oncogenic effects seen in treated primary PCa cells. Clorgyline treatment of mice bearing VCaP xenografts slowed tumor growth and induced transcriptome changes similar to those noted in vitro[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.20mL

3.24mL

1.62mL

32.40mL

6.48mL

3.24mL

参考文献

[1]Inoue H, Castagnoli K, et al. Species-dependent differences in monoamine oxidase A and B-catalyzed oxidation of various C4 substituted 1-methyl-4-phenyl-1,2,3, 6-tetrahydropyridinyl derivatives. J Pharmacol Exp Ther. 1999 Nov;291(2):856-64.

[2]Murphy DL, Karoum F, et al. Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (clorgyline) or MAO-B (selegiline and pargyline). J Neural Transm Suppl. 1998;52:39-48.

[3]Sağlık BN, Cebeci O, Acar Çevik U, Osmaniye D, Levent S, Kaya Çavuşoğlu B, Ilgın S, Özkay Y, Kaplancıklı ZA. Design, Synthesis, In Vitro and In Silico Studies of New Thiazolylhydrazine-Piperazine Derivatives as Selective MAO-A Inhibitors. Molecules. 2020 Sep 22;25(18):4342

[4]Shih JC. Monoamine oxidase isoenzymes: genes, functions and targets for behavior and cancer therapy. J Neural Transm (Vienna). 2018 Nov;125(11):1553-1566

[5]Li PC, Siddiqi IN, Mottok A, Loo EY, Wu CH, Cozen W, Steidl C, Shih JC. Monoamine oxidase A is highly expressed in classical Hodgkin lymphoma. J Pathol. 2017 Oct;243(2):220-229

[6]Lam CS, Li JJ, Tipoe GL, Youdim MBH, Fung ML. Monoamine oxidase A upregulated by chronic intermittent hypoxia activates indoleamine 2,3-dioxygenase and neurodegeneration. PLoS One. 2017 Jun 9;12(6):e0177940

[7]Flamand V, Zhao H, Peehl DM. Targeting monoamine oxidase A in advanced prostate cancer. J Cancer Res Clin Oncol. 2010 Nov;136(11):1761-71