| Field | Specification |
|---|---|
| Alternative names | BAY 85-3934 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C13H14N8O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Molidustat, also known as BAY 85-3934, is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), with IC50 values of 480 nM, 280 nM, and 450 nM against PHD1, PHD2, and PHD3, respectively. It can raise circulating erythropoietin (EPO) toward near-normal physiological levels and can be used in research on renal anemia[1][2]. It is supplied as a white to off-white solid (C13H14N8O2, MW 314.30) at 99.70% purity.
Physical & Chemical Properties
| CAS Number | 1154028-82-6 |
|---|---|
| Molecular Formula | C13H14N8O2 |
| Molecular Weight | 314.30 g/mol |
| Purity | 99.70% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C1C(N2N=NC=C2)=CNN1C3=NC=NC(N4CCOCC4)=C3 |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 5 mg/mL (15.91 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 480 nM (PHD1), 280 nM (PHD2), 450 nM (PHD3)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 5 mg/mL (15.91 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 0.5 mg/mL (1.59 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (5.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 0.5 mg/mL (1.59 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (5.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 0.5 mg/mL (1.59 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (5.0 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 4
| Composition | 0.5% CMC-Na/saline water |
|---|---|
| Result | 10 mg/mL (31.82 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
In HeLa cells, Molidustat (BAY 85-3934) (5 μM; 20 min) suffices to induce detectable HIF-1α levels. Molidustat induces, in a cell reporter assay, expression of a firefly luciferase reporter gene driven by a hypoxia response element promoter, with a mean (± SD) EC50 of 8.4 μM (n=4)[1].
In Vivo
Molidustat (BAY 85-3934) stabilizes the hypoxia-inducible factor (HIF) and thereby increases erythropoietin (EPO) dose-dependently in Wistar rats receiving 0.5-5 mg/kg orally once daily for 26 days, and in cynomolgus monkeys receiving 0.5-1.5mg/kg once daily for 5 days[1]. Molidustat (0.5-10 mg/kg; orally; five times weekly) can normalize blood pressure in rat models of chronic kidney disease (CKD), and renal anemia is effectively alleviated in rats with impaired renal function[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[1]
Rats: Dissolve BAY 85-3934 in ethanol:Solutol HS 15:water (10:20:70). In a 26-day repeat-dose experiment, administer vehicle or BAY 85-3934 at 0.5 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5 mg/kg to male Wistar rats (240–340 g in body weight). Also compare the efficacy of BAY 85-3934 (2.5 mg/kg, once-daily, oral) against rhEPO given by s.c. injection twice weekly at 25 IU/kg, 50 IU/kg, and 100 IU/kg. Determine the time-course of EPO mRNA expression and plasma EPO induction at baseline, at 0.5 h, 1 h, and 2 h, and again at 4 h, 6 h, and 8 h after a single oral dose of BAY 85-3934 (5 mg/kg)[1].
Monkey: Prepare BAY 85-3934 as a solution in 0.5% tylose. Administer 0.5 mg/kg and 1.5 mg/kg doses to male and female cynomolgus monkeys (2.8–5.6 kg in body weight), with dosing times of 0 h, 24 h, 48 h, 72 h, and 96 h. Collect blood samples at 7 h, 31 h, and 55 h, then at 79 h, 103 h, and 168 h. Also evaluate erythropoietic parameters following a 2-week treatment period in which rhEPO (100 IU/kg, twice weekly, at days 1, 4, 8, and 11) is given s.c. together with BAY 85-3934 (1.5 mg/kg) once daily[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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The transcriptional repressor Fli1 inhibits proteostasis during nutrient stress to limit NK cell persistence in solid tumors. Immunity 2026 Feb 18:S1074-7613(26)00035-X. PMID: 41713422
Hypoxic and pharmacological activation of HIF inhibits SARS-CoV-2 infection of lung epithelial cells. Cell Rep 2021 Apr 20;35(3):109020. PMID: 33852916
Excipient of paclitaxel induces metabolic dysregulation and unfolded protein response. iScience 2021 Sep 25;24(10):103170. PMID: 34646996
Baicalin inhibits macrophage glycolysis and succinate-driven HIF-1α signaling by targeting PKM2 to alleviate RSV-induced inflammation. Microb Pathog 2026 Apr:213:108291. PMID: 41544903
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. J Pharm Biomed Anal 2021 Feb 20:195:113870. PMID: 33453569
Simultaneous detection of three hypoxia-inducible factor stabilizers-molidustat, roxadustat, and vadadustat-in multiple keratinized matrices and its application in a doping context. Drug Test Anal 2025 May;17(5):647-654. PMID: 38992954
Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. Biochem Biophys Res Commun 2018 Sep 3;503(1):297-303.
bioRxiv. 2023 Nov 2.
