Hypoxia inducible factor (HIF) is the major transcription factor involved in erythropoietin gene expression. Because oxygen-dependent degradation of the α subunit of HIF suppresses erythropoietin expression, stimulation of erythropoiesis by agents that prevent degradation of HIF has been one strategy for managing anemia.{26059} BAY-85-3934 stabilizes HIF from degradation in the proteasome by inhibiting HIF-1α prolyl hydroxylase (IC50 = 0.49 µM).{26060} Inhibition of HIF prolyl hydroxylase by BAY-85-3934 has been shown to increase endogenous production of erythropoietin.{26060} This compound has been investigated in clinical trial for treatment of patients with anemia associated with chronic kidney disease and/or end-stage renal disease.{26060}
产品描述
Stabilizes HIF from degradation in the proteasome and increases endogenous production of erythropoietin by inhibiting HIF-1α prolyl hydroxylase (IC50 = 0.49 µM); investigated in clinical trial for treatment of patients with anemia associated with chronic kidney disease and/or end-stage renal disease
