Name: Molidustat (BAY 85-3934)
Brand: Selleck Chemicals
SKU: S8138
Availability: InStock
Rating: 5 (14 reviews)

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Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src FLT FLT3 HER2 Bcr-Abl
Other HIF Inhibitors	PT2399 PX-478 Dihydrochloride BAY 87-2243 KC7F2 Lificiguat (YC-1) IOX2 CAY10585 (LW 6) PT2385 IDF-11774 MK-8617

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (31.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	314.30	Formula	C₁₃H₁₄N₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1154028-82-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4

Mechanism of Action

Targets/IC₅₀/Ki	PHD2 (Cell-free assay) 280 nM PHD3 (Cell-free assay) 450 nM PHD1 (Cell-free assay) 480 nM
In vitro	In vitro, Molidustat (BAY 85-3934) induces the transcription of hypoxia-sensitive genes in HeLa, A549, and Hep3B cells.
Kinase Assay	Prolyl hydroxylase assay
Kinase 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 Molidustat (BAY 85-3934) 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 for this compound are determined after curve fitting using GraphPad Prism software applying the four-parameter logistic equation to the data sets.
In vivo	In healthy Wistar rats and cynomolgus monkeys, Molidustat (BAY 85-3934) (1.5 mg/kg, p.o.) induces dose-dependent production of EPO and erythropoiesis. In rats with induced renal anemiabe, this compound (5 mg/kg, p.o.) is also effective in raising hematocrit levels while stimulating endogenous EPO production without hypertensive effects.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25392999/ [2] https://pubmed.ncbi.nlm.nih.gov/33852916/

Applications

Methods	Biomarkers	Images	PMID
Western blot	HIF-1α		25392999

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Molidustat (BAY 85-3934) HIF modulator

Chemical Structure

Molecular Weight: 314.30