Molidustat (BAY85-3934)

- Overview
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    Background
    
    Molidustat (BAY85-3934)Description:IC50: 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively.Oxygen sensing via hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) is the dominant regulatory mechanism of erythropoietin (EPO) expression. In chronic kidney disease (CKD), impaired EPO expression causes anemia, which can be treated by supplementation with recombinant human EPO (rhEPO). Molidustat (BAY85-3934) is a novel HIF-PH inhibitor. In vitro: The IC50 values were found to be dependent on the 2-oxoglutarate concentration in the reaction buffer. By lowering the 2-oxoglutarate concentration from 20 μM to 0.3 μM, the potency of the test compound increased up to 10-fold. Variation of the concentrations of Fe2+ and ascorbate in the reaction buffer by factors of 30 and 200, respectively, did not alter the potency of the inhibitor by more than 2-fold [1]. In vivo: In repeat dosing of BAY 85-3934, hemoglobin levels were increased compared with animals in vehicle group, while endogenous EPO remained within the normal physiological range. BAY 85-3934 therapy was also effective in the treatment of renal anemia in rats with impaired kidney function and, unlike treatment with rhEPO, resulted in normalization of hypertensive blood pressure in a rat model of CKD [1]. Clinical trial: Clinical studies are still ongoing to investigate the effects of BAY 85-3934 therapy in patients with renal anemia (https://clinicaltrials.gov/ct2/show/NCT01332942?term=Molidustat&rank=2).
- Properties
  - Alternative Name
    
    2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one
    
    CAS Number
    
    1154028-82-6
    
    Molecular Formula
    
    C13H14N8O2
    
    Molecular Weight
    
    314.3
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥5.68 mg/mL in DMF
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Shaojun Wu, Ying Zhang, et al. "Septin4 promotes cardiomyocytes apoptosis by enhancing the VHL-mediated degradation of HIF-1α." Cell Death Discov. 2021 Jul 6;7(1):172. PMID:34230460
    2. Vijesh J. Bhute, James Harte, et al. "Mannose binding lectin is hydroxylated by collagen prolyl-4-hydroxylase and inhibited by some PHD inhibitors." Kidney360. April 3, 2020.

Molidustat (BAY85-3934)

Background

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