Home Angiogenesis HIF modulator Molidustat (BAY 85-3934) For research use only.

Molidustat (BAY 85-3934)

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

Molidustat (BAY 85-3934) Chemical Structure

CAS No. 1154028-82-6

Purity & Quality Control

Molidustat (BAY 85-3934) Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

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

In vitro, Molidustat induces the transcription of hypoxia-sensitive genes in HeLa, A549, and Hep3B cells. [1]
Kinase Assay Prolyl hydroxylase assay
Biotinylated HIF-1α 556–574 (biotinyl-DLDLEMLAPYIPMDDDFQL) is bound to white 96-well NeutrAvidin high binding capacity plates, which are pre-blocked with Blocker Casein and subsequently blocked with 1 mM biotin. The immobilized peptide substrate is incubated with the appropriate amount of HIF-PH in buffer containing 20 mM Tris (pH 7.5), 5 mM KCl, 1.5 mM MgCl2, 20 µM 2-oxoglutarate, 10 µM FeSO4, 2 mM ascorbate, 4% protease inhibitors without EDTA in a final volume of 100 µl, with or without test compound added at appropriate concentrations. The reaction time is 60 min. To stop the reaction, plates are washed three times with wash buffer. Hydroxylated biotinyl-HIF-1α 556–574 is incubated with Eu-VBC in 100 µl binding buffer (50 mM Tris [pH 7.5], 120 mM NaCl) for 60 min at room temperature. After washing six times with DELFIA wash buffer and adding 100 µl enhancer solution, the amount of bound VBC is determined by measuring time-resolved fluorescence with a Tecan infinite M200 plate reader. Measurements are taken in triplicate or more, and results are expressed as means ± SEM. IC50 values are determined after curve fitting using GraphPad Prism software applying the four-parameter logistic equation to the data sets.
Cell Research Cell lines Calu-3 cells
Concentrations 6 μM
Incubation Time 24 h
Method

Cells were treated with various concentrations of drug for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot HIF-1α 25392999
In Vivo
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 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]
Animal Research Animal Models Rats with induced renal anemia
Dosages 5 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03418168 Completed
Anemia|Renal Insufficiency Chronic
Bayer
 February 22 2018 Phase 3
NCT03351166 Completed
Anemia|Renal Insufficiency Chronic
Bayer
 January 22 2018 Phase 3
NCT03350347 Completed
Anemia|Renal Insufficiency Chronic
Bayer
 December 13 2017 Phase 3
NCT02312973 Completed
Renal Insufficiency Chronic
Bayer
 January 14 2015 Phase 1
NCT01458028 Completed
Anemia
Bayer
 September 2011 Phase 1
NCT01332942 Completed
Anemia
Bayer
 April 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 314.30 Formula

C13H14N8O2
CAS No. 1154028-82-6 SDF Download Molidustat (BAY 85-3934) SDF
Smiles C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 10 mg/mL ( (31.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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