Topiroxostat

Topiroxostat is an inhibitor of xanthine oxidoreductase (IC50 = 5.3 nM). It inhibits ATP-binding cassette transporter 2 (ABCG2) in isolated human plasma (IC50 = 0.18 µM). Topiroxostat (5 µM) also increases LPS-induced decreases in B cell lymphoma 2 (Bcl-2) levels and decreases LPS-induced increases of Bax and cleaved caspase-3 levels in H9c2 rat cardiomyocytes. Chronic administration of topiroxostat results in the presence of urinary xanthine crystals and induces nephropathy in rats when administered at doses of 0.2 and 1 mg/kg, respectively. Formulations containing topiroxostat have been used in the treatment of gout and hyperuricemia.Formal Name: 4-[3-(4-pyridinyl)-1H-1,2,4-triazol-5-yl]-2-pyridinecarbonitrile. CAS Number: 577778-58-6. Synonyms: FYX-051. Molecular Formula: C13H8N6. Formula Weight: 248.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/mL, DMF:PBS (pH 7.2) (1:5): 0.16 mg/mL, DMSO: 10 mg/mL. lambdamax: 208, 272 nm. SMILES: N#CC1=CC(C2=NN=C(C3=CC=NC=C3)N2)=CC=N1. InChi Code: InChI=1S/C13H8N6/c14-8-11-7-10(3-6-16-11)13-17-12(18-19-13)9-1-4-15-5-2-9/h1-7H,(H,17,18,19). InChi Key: UBVZQGOVTLIHLH-UHFFFAOYSA-N.