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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETranylcypromine hemisulfateCat. No.: HY-B1496CAS No.: 13492-01-8Synonyms: dl-Tranylcypromine hemisulfate; trans-2-Phenylcyclopropylamine hemisulfate salt分式: CHNOS.分量: 182.23作靶點: Monoamine Oxidase; Histone Demethylase作通路: Neurona
2、l Signaling; Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 25 mg/mL (137.19 mM; Need ultrasonic)DMSO : 5 mg/mL (27.44 mM; ultrasonic and warming and heat to 60C)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 5.4876 mL 27.4379 mL 54.8757 mL5 mM 1
3、.0975 mL 5.4876 mL 10.9751 mL10 mM 0.5488 mL 2.7438 mL 5.4876 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Tranylcypromine hemisulfate種于治療抑郁癥的不可逆,選擇性 MAO 抑制劑。體外研究Tranylcypromine (10 nM to 10 M) exerts neuroprotective effects against toxicity induced by human A(1-42)oligomers
4、independently from the presence of glial cells 1. Tranylcypromine (100 M) significantly protects1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemERGCs from glutamate neurotoxicity-induced apoptosis as well as apoptosis induced by oxidative stress.Tranylcypromine promotes mitogen-activated protein kin
5、ase 12 (p38 MAPK) expression under conditions ofglutamate (Glu)-induced stress. Besides, tranylcypromine contributes to RGC survival via alterations of p38MAPK activity 3.體內(nèi)研究 Tranylcypromine treatment significantly and substantially reduces the lesion size and improves generalizedhyperalgesia in a
6、dose-dependent fashion in mice with induced endometriosis. In addition, tranylcyprominetreatment results in reduced immunoreactivity to biomarkers of proliferation, angiogenesis, and H3K4methylation, leading to arrested EMT and lesion growth 2. Tranylcypromine (500 mM) injection exertsneuroprotectiv
7、e effects within intracellular apoptotic signaling pathways and suppresses morphologicchanges in the retina of the rat, suppresses caspase 3 activity and recovers p38 MAPK expression in theretina after NMDA-induced injury, and enhances RGC survival after retinal injury via the attenuation of NMDAneu
8、rotoxicity 3. Tranylcypromine (10 g/g) causes an approximate and significant doubling of labeled cellsin the combined brain regions examined, as detected by BrdU immunohistochemistry. Tranylcyprominecauses the greatest increase in cell proliferation in the cerebellum 4.PROTOCOLAnimal Briefly, the ra
9、ts are anesthetized with an intraperitoneal injection of a 1:1 mixture of xylazine hydrochloride (4Administration 3 mg/kg) and ketamine hydrochloride (10 mg/kg). Then, the pupil is dilated with phenylephrine hydrochlorideand tropicamide eye drops, and 20 nmol NMDA with or without tranylcypromine is
10、injected into the vitreouscavity. To assess the inhibitory effect of mitogen-activated protein kinase (MAPK), 100 nmol BIRB796 isintravitreally injected at the same time of NMDA injection. The injections are performed under a microscopeusing a 33-gauge needle connected to a microsyringe; the needle
11、is inserted approximately 1.0 mm behindthe corneal limbus. Next, either PBS (vehicle control) or 500 mM tranylcypromine (1000 nmol) mixed with 10mM NMDA (20 nmol) in a total volume of 2.0 L is injected into the vitreous cavity.MCE has not independently confirmed the accuracy of these methods. They a
12、re for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Biomaterials. 2018 Dec 6;193:30-46. Biochem Biophys Res Commun. 2019 May 14;512(4):852-858. Patent. US20180263995A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Caraci F, et al. Neuroprotective effects of the monoamine oxidase inhibitor tran
13、ylcypromine and its amide derivatives against A(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 generalizedhyperalgesia in mouse with induced endometriosis. Repro
14、d Biol Endocrinol. 2016 Apr 9;14:17.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. Tsutsumi T, et al. Potential Neuroprotective Effects of an LSD1 Inhibitor in Retinal Ganglion Cells via p38 MAPK Activity. InvestOphthalmol 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;2
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