Molidustat (BAY 85-3934)

Catalog No.S8138

Molidustat (BAY 85-3934) Chemical Structure

Molecular Weight(MW): 314.30

Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2.

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1 Customer Review

  • Western blot analysis of the indicated proteins after the treatment with BAY 85-394 (L).

    Theranostics, 2017, 7(13): 3293-3305. Molidustat (BAY 85-3934) purchased from Selleck.

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Biological Activity

Description Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2.
Targets
PHD2 [1]
(Cell-free assay)
PHD3 [1]
(Cell-free assay)
PHD1 [1]
(Cell-free assay)
280 nM 450 nM 480 nM
In vitro

In vitro, Molidustat induces the transcription of hypoxia-sensitive genes in HeLa, A549, and Hep3B cells. [1]

In vivo In healthy Wistar rats and cynomolgus monkeys, Molidustat (1.5 mg/kg, p.o.) induces dose-dependent production of EPO and erythropoiesis. In rats with gentamicin-induced renal anemiabe, Molidustat (5 mg/kg, p.o.) is also effective in raising hematocrit levels while stimulating endogenous EPO production without hypertensive effects. [1]

Protocol

Animal Research:

[1]

+ Expand
  • Animal Models: Rats with gentamicin-induced renal anemia
  • Formulation: ethanol:Solutol HS 15:water (10:20:70)
  • Dosages: 5 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMF 4 mg/mL (12.72 mM)
DMSO 3 mg/mL warmed (9.54 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 314.30
Formula

C13H14N8O2

CAS No. 1154028-82-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02312973 Completed Renal Insufficiency, Chronic Bayer January 2015 Phase 1
NCT02064426 Completed Anemia|Renal Insufficiency, Chronic Bayer March 2014 Phase 2
NCT01975818 Completed Anemia|Renal Insufficiency, Chronic Bayer October 2013 Phase 2
NCT01679587 Completed Kidney Diseases Bayer September 2012 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID