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Tranylcypromine (2-PCPA) hydrochloride

Catalog No. T1025   CAS 1986-47-6
Synonyms: Tranylcypromine (2-PCPA) HCl, SKF-385 HCl

Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl), a Monoamine Oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression.

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Tranylcypromine (2-PCPA) hydrochloride Chemical Structure
Tranylcypromine (2-PCPA) hydrochloride, CAS 1986-47-6
Pack Size Availability Price/USD Quantity
100 mg In stock $ 39.00
200 mg In stock $ 51.00
1 mL * 10 mM (in DMSO) In stock $ 39.00
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Purity: 97.19%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl), a Monoamine Oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression.
Targets&IC50 LSD1:22.3 μM, MAO-A:11.5 μM, MAO-B:7 μM
In vitro Compared with the control group, Tranylcypromine at dosages of 5 mg/kg and 10 mg/kg significantly and gradually increased muscle activity in male rats; however, a 2 mg/kg dosage of Tranylcypromine had no effect. Additionally, Tranylcypromine administered at 10 mg/kg markedly increased the number of copulatory behaviors in male rats.
In vivo In bovine aortic endothelial cells, Tranylcypromine (500 μg/mL) markedly inhibits bradykinin-induced release of arachidonic acid. Additionally, Tranylcypromine suppresses the activity of CYP2A6 (IC50: 0.42 μM) and CYP2E1 (IC50: 3 μM) in human liver microsomes (HLMs), inducing type II and cyclopropylbenzene type I difference spectra in HLMs. Nicotine metabolism mediated by CYP2A6 in HLMs is completely inhibited by R-(+)-Tranylcypromine (Ki: 0.05 μM), (±)-Tranylcypromine (Ki: 0.08 μM), and S-(-)-Tranylcypromine (Ki: 2.0 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 Tranylcypromine (2-PCPA) HCl, SKF-385 HCl
Molecular Weight 169.66
Formula C9H11N·HCl
CAS No. 1986-47-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 17 mg/mL (100 mM)

DMSO: 17 mg/mL (100 mM)

TargetMolReferences 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 Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Approved Drug Library Anti-Neurodegenerative Disease Compound Library FDA-Approved Drug Library Mitochondria-Targeted Compound Library Epigenetics Compound Library

Related Products

Related compounds with same targets
T-3775440 hydrochloride JIB-04 CP2 JQKD82 L-2-Hydroxyglutaric acid disodium (rel)-Tranylcypromine D5 hydrochloride T-448 LSD1-UM-109

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Keywords

Tranylcypromine (2-PCPA) hydrochloride 1986-47-6 Chromatin/Epigenetic Metabolism Neuroscience MAO Histone Demethylase Tranylcypromine (2-PCPA) Hydrochloride Tranylcypromine (2-PCPA) HCl Tranylcypromine (2PCPA) hydrochloride SKF-385 HCl Tranylcypromine (2 PCPA) hydrochloride inhibitor inhibit

 

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