Tranylcypromine (2-PCPA) HCl

Catalog No.S4246 Synonyms: SKF-385 HCl

Tranylcypromine (2-PCPA) HCl Chemical Structure

Molecular Weight(MW): 169.65

Tranylcypromine 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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Cited by 4 Publications

1 Customer Review

  • Brain cellular proliferation and apoptosis rates were analyzed by Ki67. Scale bars: 200 µm.

    Front Neurol, 2017, 8:626. Tranylcypromine (2-PCPA) HCl purchased from Selleck.

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Biological Activity

Description Tranylcypromine 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

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 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]

Protocol

Solubility (25°C)

In vitro DMSO 33 mg/mL (194.51 mM)
Water 33 mg/mL (194.51 mM)
Ethanol 33 mg/mL (194.51 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 169.65
Formula

C9H12ClN

CAS No. 1986-47-6
Storage powder
in solvent
Synonyms SKF-385 HCl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID