Tranylcypromine HCl

Synonyms: 2-PCPA HCl, SKF-385 HCl

Tranylcypromine HCl is a monoamine oxidase inhibitor, which inhibits CYP2A6 with Ki of 0.08 μM and 0.2 μM in cDNA-expressing microsomes and Human Liver Microsomes, respectively.

Tranylcypromine HCl Chemical Structure

Tranylcypromine HCl Chemical Structure

CAS: 1986-47-6

Selleck's Tranylcypromine HCl has been cited by 16 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.91%
99.91

Choose Selective MAO Inhibitors

Biological Activity

Description Tranylcypromine HCl is a monoamine oxidase inhibitor, which inhibits CYP2A6 with Ki of 0.08 μM and 0.2 μM in cDNA-expressing microsomes and Human Liver Microsomes, respectively.
Targets
MAO-B [5]
(Cell-free assay)
MAO-A [1]
(Cell-free assay)
LSD1 [5]
(Cell-free assay)
7 μM 11.5 μM 22.3 μM
In vitro
In vitro R-(+)-Tranylcypromine, (±)-Tranylcypromine, and S-(−)-Tranylcypromine competitively inhibits CYP2A6-mediated metabolism of nicotine with apparent Ki values of 0.05 μM, 0.08 μM, and 2.0 μM, respectively, in human liver microsomes. [1] Tranylcypromine (500 μg/mL) severely inhibits bradykinin-stimulated arachidonic acid release in calf aortic endothelial cells. [2] Tranylcypromine inhibits CYP2A6 and CYP2E1 activity with IC50 of 0.42 μM and 3 μM, respectively, in human liver microsomes. Tranylcypromine induces type II and cyclopropylbenzene type I difference spectrum in human liver microsomes. [3]
In Vivo
In vivo Tranylcypromine injection leads to a large, slow increase in motor activity at 5 mg/kg and 10 mg/kg compared with the saline control in male rats, although 2 mg/kg Tranylcypromine does not induce an increase. Tranylcypromine (10 mg/kg) also causes significant decreases in the number of rearing behaviors in male rats. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04841798 Completed Major Depressive Disorder|Treatment Resistant Depression Centre for Addiction and Mental Health April 15 2021 Not Applicable

Chemical lnformation & Solubility

Molecular Weight 169.65 Formula

C9H12ClN

CAS No. 1986-47-6 SDF Download Tranylcypromine HCl SDF
Smiles C1C(C1N)C2=CC=CC=C2.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 34 mg/mL ( (200.41 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 34 mg/mL

Ethanol : 34 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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