| 货号 | 21267-100mg |
| 描述 | Topiroxostat is an inhibitor of xanthine oxidoreductase (IC50 = 5.3 nM), an enzyme that converts xanthine to urate.1 Formulations containing topiroxostat are effective in vivo, lowering urate levels in the serum of patients with hyperuricemia.2 In rats, but not primates, topiroxostat treatment results in the formation of xanthine crystals, resulting in nephritis.3,4 Topiroxostat also inhibits ATP-binding cassette transporter G2 (ABCG2; IC50 = 0.18 µM), a high-capacity urate transporter that functions in both renal and extrarenal urate secretion.5 |
| 别名 | FYX-051; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sato, T.,Ashizawa, N.,Matsumoto, K., et al. Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia. Bioor. Med. Chem. Lett. 19(21), 6225-6229 (2009). 2.Hosoya, T.,Sasaki, T. and Ohashi, T. Clinical efficacy and safety of topiroxostat in Japanese hyperuricemic patients with or without gout: A randomized, double-blinded, controlled phase 2b study. Clin. Rheumatol. Epub ahead of print, (2016). 3.Shimo, T.,Ashizawa, N.,Matsumoto, K., et al. Simultaneous treatment with citrate prevents nephropathy induced by FYX-051, a xanthine oxidoreductase inhibitor, in rats. Toxicol. Sci. 87(1), 267-276 (2005). 4.Shimo, T.,Ashizawa, N.,Moto, M., et al. FYX-051, a xanthine oxidoreductase inhibitor, induces nephropathy in rats, but not in monkeys. Toxicol. Pathol. 37(4), 438-445 (2009). 5.Miyata, H.,Takada, T.,Toyoda, Y., et al. Identification of febuxostat as a new strong ABCG2 inhibitor: Potential applications and risks in clinical situations. Front. Pharmacol. 7(518), (2016). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 248.2 |
| 分子式 | C13H8N6 |
| CAS号 | 577778-58-6 |
| 稳定性 | ≥ 2 years |
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