Leflunomide

Leflunomide is a synthetic isoxazol and a prodrug form of A-771726 (Cay-14404), a dihydroorotate dehydrogenase inhibitor. Leflunomide inhibits de novo pyrimidine synthesis to regulate T lymphocyte progression through the cell cycle. It inhibits proliferation and activation of T cells when used at concentrations of 25 and 100 µM, respectively, for naïve and memory CD4+ T cells. It also reduces the production of Th1 effector cells and increases differentiation of Th2 cells in vitro and in splenocytes isolated from KLH-immunized mice. Leflunomide (35 mg/kg per day) reduces and prevents inflammation in a proteoglycan-induced mouse model of rheumatoid arthritis. Formulations containing leflunomide have been used in the treatment of active rheumatoid arthritis.Formal Name: 5-methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide. CAS Number: 75706-12-6. Synonyms: HW 486, SU 101. Molecular Formula: C12H9F3N2O2. Formula Weight: 270.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 16.7 mg/ml, Ethanol: 20 mg/ml. lambdamax: 206, 262 nm. SMILES: O=C(C1=C(C)ON=C1)NC2=CC=C(C(F)(F)F)C=C2. InChi Code: InChI=1S/C12H9F3N2O2/c1-7-10(6-16-19-7)11(18)17-9-4-2-8(3-5-9)12(13,14)15/h2-6H,1H3,(H,17,18). InChi Key: VHOGYURTWQBHIL-UHFFFAOYSA-N.