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).
| Molecular Weight | 270.21 |
| Formula | C12H9F3N2O2 |
| CAS Number | 75706-12-6 |
| Solubility (25°C) | DMSO 40 mg/mL Ethanol 10 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.
| Related DHODH Products |
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| DHODH-IN-13
DHODH-IN-13 is a hydroxyfurazan analog of A771726 and a dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for hepatic DHODH in rats.DHODH-IN-13 can be used in rheumatoid arthritis-related studies. |
| DHODH-IN-12
DHODH-IN-12 is a Leflunomide derivative and a weak inhibitor of dihydroorotic acid dehydrogenase (DHODH), with a pKa of 5.07. |
| hDHODH-IN-5
hDHODH-IN-5 is a human dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 0.91 μM. hDHODH-IN-7 induces differentiation of acute myeloid leukemia cells. |
| DHODH-IN-8
DHODH-IN-8 is an inhibitor of human and Plasmodium falciparum dihydroorotic acid dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM and Ki of 0.016 μM and 5.6 μM, respectively.DHODH-IN-8 exhibits antimalarial activity. |
| DHODH-IN-14
DHODH-IN-14 is a hydroxyfurazan analog of A771726 and a dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for hepatic DHODH in rats.DHODH-IN-14 can be used in rheumatoid arthritis-related studies. |
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