Tranylcypromine (2-PCPA) hydrochloride

SKU: orb1225767

Description

Tranylcypromine is a drug of the substituted phenethylamine and amphetamine classes which acts as a monoamine oxidase inhibitor (MAOI)—it is a nonselective and irreversible inhibitor of the enzyme monoamine oxidase (MAO).(In Vitro):Tranylcypromine hydrochlorid (50 μM-5 mM; 1 h or 12-14 h) inhibits histone and nucleosomal demethylation.Tranylcypromine hydrochlorid (2 μM; 3 h) shows a specific derepression of OCT4 transcription.Tranylcypromine hydrochlorid (0-100 μM; 15 min) shows IC50 values of 20.7, 2.3 and 0.95 μM for LSD1, MAO A and MAO B, respectively.Tranylcypromine hydrochlorid (0-800 μM) shows Ki values of 242.7, 101.9 and 16 μM for LSD1, MAO A and MAO B, respectively.(In Vivo):Tranylcypromine hydrochlorid (3 mg/kg; i.p. once daily for 3 days) decreases LPS-mediated microglial activation and proinflammatory cytokine COX-2 and IL-6 levels in wild-type mice.Tranylcypromine hydrochlorid (3 mg/kg; i.p. once daily for 7 days) down-regulates Aβ-mediate microglial activation in 5xFAD mice.

Images & Validation

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Key Properties

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CAS Number	1986-47-6
MW	169.66
Purity	>98% (HPLC)
Formula	C₉H₁₁N·HCl
SMILES	N[C@H]1[C@H](C2=CC=CC=C2)C1.[H]Cl
Target	MAO
Solubility	Ethanol: 33 mg/mL (194.51 mM); Water: 33 mg/mL (194.51 mM); DMSO: 33 mg/mL (194.51 mM)

Bioactivity

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In Vivo

Tranylcypromine hydrochlorid (3 mg/kg; i.p. once daily for 3 days) decreases LPS-mediated microglial activation and proinflammatory cytokine COX-2 and IL-6 levels in wild-type mice. Tranylcypromine hydrochlorid (3 mg/kg; i.p. once daily for 7 days) down-regulates Aβ-mediate microglial activation in 5xFAD mice. Animal model: Wild-type mice. Dosage: 3 mg/kg. Administration: Intraperitoneal injection; 3 mg/kg once daily for 3 days. Result: Significantly down-regulated LPS-stimulated microglial activation in the cortex and Hippocampus, and LPS-induced astrocyte activation only in the cortex. Reduced LPS-induced COX-2 levels in hippocampus CA1, decreased LPS-evoked IL-6 levels in the cortex and hippocampus CA1 and suppressed LPS-mediated IL-1β levels in the cortex. Animal model: 5xFAD mice. Dosage: 3 mg/kg. Administration: Intraperitoneal injection; 3 mg/kg once daily for 7 days. Result: Differentially regulated microglial and astrocyte activation in this mouse model of AD.

In Vitro

Tranylcypromine hydrochlorid (50 μM-5 mM; 1 h or 12-14 h) inhibits histone and nucleosomal demethylation. Tranylcypromine hydrochlorid (2 μM; 3 h) shows a specific derepression of OCT4 transcription. Tranylcypromine hydrochlorid (0-100 μM; 15 min) shows IC50 values of 20.7, 2.3 and 0.95 μM for LSD1, MAO A and MAO B, respectively. Tranylcypromine hydrochlorid (0-800 μM) shows Ki values of 242.7, 101.9 and 16 μM for LSD1, MAO A and MAO B, respectively. Western blot analysis. Cell line: Sf21 insect cell line. Concentration: 50 μM, 200 μM, 1 mM and 5 mM. Incubation time: 12-14 hours or 1 hour. Result: Showed inhibitory activities of histone H3K4 demethylation and nucleosomal demethylation. RT-PCR Cell line: P19 EC cell line. Concentration: 2 μM. Incubation time: 3 hours. Result: Decreased Oct4 mRNA levels.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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trans-2-Phenylcyclopropylamine | Tranylcypromine

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Gene Symbol

MAO

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