Description
Tranylcypromine HCl (2-PCPA, SKF-385, Parnate) 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.
Product information
CAS Number: 1986-47-6
Molecular Weight: 169.65
Formula: C9H12ClN
Chemical Name: 2-phenylcyclopropan-1-amine hydrochloride
Smiles: Cl.N[C@@H]1C[C@H]1C1C=CC=CC=1
InChiKey: ZPEFMSTTZXJOTM-OULXEKPRSA-N
InChi: InChI=1S/C9H11N.ClH/c10-9-6-8(9)7-4-2-1-3-5-7;/h1-5,8-9H,6,10H2;1H/t8-,9+;/m0./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 17 mg/mL (100 mM) water: 17 mg/mL (100 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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:
- Zhang W, et al. Drug Metab Dispos, 2001, 29(6), 897-902.
- Hong SL, et al. J Biol Chem, 1980, 255(20), 9538-9540.
- Taavitsainen P, et al. Drug Metab Dispos, 2001, 29(3), 217-222.
Products are for research use only. Not for human use.
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