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HomeProduct name listMolidustat(BAY 85-3934)

Molidustat(BAY 85-3934)

  • CAS NO.:1154028-82-6
  • Empirical Formula: C13H14N8O2
  • Molecular Weight: 314.3
  • MDL number: MFCD28411428
  • EINECS: 815-038-0
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-07-02 08:55:16
Molidustat(BAY 85-3934) Structural

What is Molidustat(BAY 85-3934)?

Description

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. BAY 85-3934 stabilizes HIF from degradation in the proteasome by inhibiting HIF-1α prolyl hydroxylase (IC50 = 0.49 μM). Inhibition of HIF prolyl hydroxylase by BAY 85-3934 has been shown to increase endogenous production of erythropoietin. 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.

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].

References

[1] flamme i, oehme f, ellinghaus p, jeske m, keldenich j, thuss u. mimicking hypoxia to treat anemia: hif-stabilizer bay 85-3934 (molidustat) stimulates erythropoietin production without hypertensive effects. plos one. 2014 nov 13;9(11):e111838.

Properties of Molidustat(BAY 85-3934)

Boiling point: 589.2±60.0 °C(Predicted)
Density  1.67±0.1 g/cm3(Predicted)
storage temp.  Store at -20°C
solubility  insoluble in EtOH; insoluble in H2O; ≥5.68 mg/mL in DMF
form  solid
pka 5.38±0.37(Predicted)
color  White to off-white

Safety information for Molidustat(BAY 85-3934)

Computed Descriptors for Molidustat(BAY 85-3934)

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