Leflunomide
Katalog-Nummer M2229-500mg
Size : 500mg
Marke : AbMole Bioscience
HWA486; RS-34821; SU101
Quality Control & Documentation
Biological Activity
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).
Chemical Information
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 |
Conversion of different model animals based on BSA (PMID: 27057123)
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.
References
[1] Davis JP, et al. Biochemistry. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase.
[2] Xu X, et al. J Biol Chem. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide.