[CAS NO. 1986-47-6] Tranylcypromine (2-PCPA) HCl

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PRODUCTS SPECIFICATIONS [1986-47-6]

Catalog

SLK-S4246

Brand

Selleck

CAS

1986-47-6

DESCRIPTION [1986-47-6]

Overview

MDL	MFCD00063602
Molecular Weight	169.65
Molecular Formula	C9H12ClN
SMILES	N[C@H]1[C@H](C2=CC=CC=C2)C1.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	5.8945 mL	29.4724 mL	58.9449 mL
5 mM	1.1789 mL	5.8945 mL	11.7890 mL
10 mM	0.5894 mL	2.9472 mL	5.8945 mL
50 mM	0.1179 mL	0.5894 mL	1.1789 mL

Description

Tranylcypromine HCl (2-PCPA, SKF-385, Parnate) is a inhibitor, which inhibits CYP2A6 with 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. 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

[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.
[5] Ji YY, et al. Eur J Med Chem. 2017, 141:101-112.