Leflunomide is an inhibitor of dihydroorotate dehydrogenase with IC50 of 2.5 μM. Leflunomide inhibits de novo pyrimidine synthesis in human T-cells in vitro. Leflunomide also inhibits lymphocyte proliferation. The inhibition of human DHODH by A77 1726, the active metabolite of leflunomide, occurs at levels (approximately 600 nM) that are achieved during treatment of rheumatoid arthritis (RA).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL
Ethanol 10 mg/mL
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase.
Davis JP, et al. Biochemistry. 1996 Jan 30;35(4):1270-3. PMID: 8573583.
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide.
Xu X, et al. J Biol Chem. 1995 May 26;270(21):12398-403. PMID: 7759480.
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