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Tranylcypromine HCl MAO inhibitor

Cat.No.S4246

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.
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Quality Control

Batch: Purity: 99.91%
99.91

Solubility

In vitro
Batch:

DMSO : 34 mg/mL (200.41 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 34 mg/mL

Ethanol : 34 mg/mL

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In vivo
Batch:

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 169.65 Formula

C9H12ClN

Storage (From the date of receipt)
CAS No. 1986-47-6 Download SDF Storage of Stock Solutions

Synonyms 2-PCPA HCl, SKF-385 HCl SMILES C1C(C1N)C2=CC=CC=C2.Cl

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Mechanism of Action

Targets/IC50/Ki
MAO-B
(Cell-free assay)
7 μM
MAO-A
(Cell-free assay)
11.5 μM
LSD1
(Cell-free assay)
22.3 μM
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. Tranylcypromine (500 μg/mL) severely inhibits bradykinin-stimulated arachidonic acid release in calf aortic endothelial cells. 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.
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15289160/
  • [5] https://pubmed.ncbi.nlm.nih.gov/29031059/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04841798 Completed
Major Depressive Disorder|Treatment Resistant Depression
Centre for Addiction and Mental Health
2021-04-15 Not Applicable
NCT02717884 UNKNOWN
Acute Myeloid Leukemia; Myelodysplastic Syndrome
Michael Luebbert
2015-05 PHASE1; PHASE2
NCT02273102 COMPLETED
Acute Myelogenous Leukemia; Myelodysplastic Syndromes; Leukemia
University of Miami
2015-03-02 PHASE1
NCT02261779 UNKNOWN
AML
Martin-Luther-Universität Halle-Wittenberg
2014-09 PHASE1; PHASE2
NCT02374567 TERMINATED
Dementia; Depression; Schizophrenia; Psychosomatic Disorders; Anxiety Disorders
Hannover Medical School
2015-01 PHASE3
NCT00223691 COMPLETED
Autonomic Failure; Orthostatic Hypotension
Vanderbilt University
2002-03 PHASE1

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