Molidustat (BAY 85-3934)

Catalog No.S8138

For research use only.

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.

Molidustat (BAY 85-3934) Chemical Structure

CAS No. 1154028-82-6

Selleck's Molidustat (BAY 85-3934) has been cited by 8 Publications

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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]

Assay
Methods Test Index PMID
Western blot HIF-1α 25392999
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 (from reference)

Animal Research:

[1]

  • Animal Models: Rats with gentamicin-induced renal anemia
  • Dosages: 5 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 314.30
Formula

C13H14N8O2

CAS No. 1154028-82-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03418168 Completed Drug: Molidustat (BAY85-3934) Anemia|Renal Insufficiency Chronic Bayer February 22 2018 Phase 3
NCT03351166 Completed Drug: Molidustat (BAY85-3934) Anemia|Renal Insufficiency Chronic Bayer January 22 2018 Phase 3
NCT03350347 Completed Drug: Molidustat (BAY85-3934)|Drug: Darbepoetin alfa Anemia|Renal Insufficiency Chronic Bayer December 13 2017 Phase 3
NCT02312973 Completed Drug: Molidustat(BAY85-3934) Renal Insufficiency Chronic Bayer January 14 2015 Phase 1
NCT01458028 Completed Drug: BAY85-3934|Drug: Placebo Anemia Bayer September 2011 Phase 1
NCT01332942 Completed Drug: BAY85-3934 Anemia Bayer April 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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