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

BAY 85-3934 – 5 mg

Brand:
Cayman
CAS:
1154028-82-6
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

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

Formal name: 1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)-3H-pyrazol-3-one

Synonyms:  Molidustat

Molecular weight: 314.3

CAS: 1154028-82-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Prolyl Hydroxylation Enzymes||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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