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Tranylcypromine (2-PCPA) hydrochloride

Catalog No. T1025   CAS 1986-47-6
Synonyms: SKF-385 HCl, Tranylcypromine (2-PCPA) HCl, 反苯环丙胺盐酸盐

Tranylcypromine Hydrochloride, a monoamine oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It is a propylamine formed from the cyclization of the side chain of amphetamine. It also is useful in panic and phobic disorders.

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Tranylcypromine (2-PCPA) hydrochloride, CAS 1986-47-6
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tranylcypromine Hydrochloride, a monoamine oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It is a propylamine formed from the cyclization of the side chain of amphetamine. It also is useful in panic and phobic disorders.
Targets&IC50 MAO-B:7 μM, LSD1:22.3 μM, MAO-A:11.5 μM
Kinase Assay PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl2, 0.5 μM cAMP or cGMP, and [3H]cAMP or [3H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration[3].
Synonyms SKF-385 HCl, Tranylcypromine (2-PCPA) HCl, 反苯环丙胺盐酸盐
Molecular Weight 169.65
Formula C9H12ClN
CAS No. 1986-47-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 17 mg/mL (100 mM)

DMSO: 17 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Zhang W, et al. Drug Metab Dispos, 2001, 29(6), 897-902. 2. Hong SL, et al. J Biol Chem, 1980, 255(20), 9538-9540. 3. Taavitsainen P, et al. Drug Metab Dispos, 2001, 29(3), 217-222. 4. Negishi T, et al. Environ Health Perspect, 2004, 112(11), 1159-1164.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Cardiovascular Disease Compound Library Inhibitor Library Drug-induced Liver Injury (DILI) Compound Library Histone Modification Compound Library Anti-Metabolism Disease Compound Library Covalent Inhibitor Library Anti-Alzheimer's Disease Compound Library Drug Repurposing Compound Library

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Keywords

Tranylcypromine (2-PCPA) hydrochloride 1986-47-6 表观遗传 代谢 神经科学 MAO Histone Demethylase Tranylcypromine (2-PCPA) HCl Tranylcypromine (2PCPA) hydrochloride SKF-385 HCl Tranylcypromine (2 PCPA) hydrochloride Inhibitor inhibitor inhibit