DesiduSTAT 是一种 HIF 羟化酶的抑制剂，摘自专利文献 WO 2014102818 A1，化合物实例 2。

Desidustat is an inhibitor of HIF hydroxylase.

In BALB/c mice, a single dose treatment of desidustat attenuated the effect of lipopolysaccharide (LPS) - or turpentine oil-induced inflammation and increased serum erythropoietin (EPO), iron, and reticulocyte count, and decreased serum hepcidin levels. In turpentine oil-induced anemia in BALB/c mice, repeated dose desidustat treatment increased hemoglobin, RBC and hematocrit in a dose related manner. In female Lewis rats, treatment with desidustat markedly reduced PGPS-induced anemia and increased hemoglobin, red blood cell (RBC) and white blood cell (WBC) count, hematocrit, serum iron and spleen iron.

Male BALB/c mice were administered turpentine oil (5 ml/kg, s.c.). In another set of experiment, animals were administered LPS (1 mg/kg, i.p.). Animals were treated with vehicle (0.25 % CMC) or desidustat (15 mg/kg, p.o.) along with either turpentine oil or LPS treatment. Animals were killed 16 h after turpentine oil and 6 h after LPS treatment. At the end of treatment, animals were bled by a retroorbital puncture. Spleen and liver tissue were collected for estimation of total iron. Serum samples were analyzed for total iron content as mentioned in the analysis section.

1616690-16-4

C16H16N2O6

332.312

DMSO:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years