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Tranylcypromine HCl 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. Tranylcypromine hydrochlorid (50 μM-5 mM; 1 h or 12-14 h) inhibits histone and nucleosomal demethylation.
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.
| Molecular Weight | 169.65 |
| Formula | C9H12ClN |
| CAS Number | 1986-47-6 |
| Solubility (25°C) | Water 60 mg/mL DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] F LEES, et al. Lancet. Tranylcypromine
[5] R M Atkinson, et al. Clin Pharmacol Ther. Tranylcypromine: a review
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