808118-40-3

Roxadustat (FG-4592) 是一种口服生物可利用的缺氧诱导因子脯氨酰羟化酶抑制剂，通过增加内源性促红细胞生成素、改善铁调节和降低铁调素来促进红细胞生成，具有潜在的抗贫血活性。

Roxadustat-D5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat (T2515) is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4,1.26,and 1.32 µM for HIF-PH1,HIF-PH2,and HIF-PH3,respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases,including lysine-specific demethylase 5A (KDM5A),KDM5B,-5C,-5D,and -6B (IC50s = >100 µM for all). Roxadustat (T2515) (10-200 µM)stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg/kg. Roxadustat (T2515)reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide,as well as a rat model of chronic kidney disease induced by 5/6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcin......

Roxadustat-13C-15N是Roxadustat (T2515)的 13C 和 15N 的标记化合物。

Roxadustat-13C2-15N是Roxadustat (T2515)的 13C 和 15N 的标记化合物。