Tranylcypromine (2-PCPA) hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tranylcypromine 是一种取代苯乙胺和安非他明类化合物，可作为单胺氧化酶抑制剂 (MAOI)。

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.

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.

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.

trans-2-Phenylcyclopropylamine | Tranylcypromine

Metabolic Enzyme/Protease

MAO

MAO

Neurological Disease

——

1986-47-6

169.66

C9H11N·HCl

>98% (HPLC)

Ethanol: 33 mg/mL (194.51 mM); Water: 33 mg/mL (194.51 mM); DMSO: 33 mg/mL (194.51 mM)

N[C@H]1[C@H](C2=CC=CC=C2)C1.[H]Cl

trans-2-Phenylcyclopropylamine Hydrochloride

(-20℃)

With Ice Pack

≥ 2 years