S82931 |
Tranylcypromine hemisulfate |
源叶(MedMol) | 99% |
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- 产品描述: Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects
- 靶点: KDM1/LSD1;HistoneDemethylase; MAO; MonoamineOxidase
- 体外研究:
Tranylcypromine (10 nM to 10 µM) exerts neuroprotective effects against toxicity induced by human Aβ(1-42) oligomers independently from the presence of glial cells. Tranylcypromine (100 μM) significantly protects RGCs from glutamate neurotoxicity-induced apoptosis as well as apoptosis induced by oxidative stress. Tranylcypromine promotes mitogen-activated protein kinase 12 (p38 MAPKγ) expression under conditions of glutamate (Glu)-induced stress. Besides, tranylcypromine contributes to RGC survival via alterations of p38 MAPKγ activity.
- 体内研究:
Tranylcypromine treatment significantly and substantially reduces the lesion size and improves generalized hyperalgesia in a dose-dependent fashion in mice with induced endometriosis. In addition, tranylcypromine treatment results in reduced immunoreactivity to biomarkers of proliferation, angiogenesis, and H3K4 methylation, leading to arrested EMT and lesion growth. Tranylcypromine (500 mM) injection exerts neuroprotective effects within intracellular apoptotic signaling pathways and suppresses morphologic changes in the retina of the rat, suppresses caspase 3 activity and recovers p38 MAPKγ expression in the retina after NMDA-induced injury, and enhances RGC survival after retinal injury via the attenuation of NMDA neurotoxicity. Tranylcypromine (10 µg/g) causes an approximate and significant doubling of labeled cells in the combined brain regions examined, as detected by BrdU immunohistochemistry. Tranylcypromine causes the greatest increase in cell proliferation in the cerebellum.
- 参考文献:
1. Caraci F, et al. Neuroprotective effects of the monoamine oxidase inhibitor tranylcypromine and its amide derivatives against Aβ(1-42)-induced toxicity. Eur J Pharmacol. 2015 Oct 5;764:256-263. 2. Sun Q, et al. Tranylcypromine, a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Reprod Biol Endocrinol. 2016 Apr 9;14:17. 3. Tsutsumi T, et al. Potential Neuroprotective Effects of an LSD1 Inhibitor in Retinal Ganglion Cells via p38 MAPK Activity. Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6461-6473. 4. Romanczyk TB, et al. The antidepressant tranylcypromine alters cellular proliferation and migration in the adult goldfish brain. Anat Rec (Hoboken). 2014 Oct;297(10):1919-26.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.744 ml 13.719 ml 27.438 ml 5 mM 0.549 ml 2.744 ml 5.488 ml 10 mM 0.274 ml 1.372 ml 2.744 ml 50 mM 0.055 ml 0.274 ml 0.549 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)