A pan-HIF-PH inhibitor
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BAY 85-3934

Item No. 15297

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)-3H-pyrazol-3-one
CAS Number
1154028-82-6
Synonyms
  • Molidustat
Molecular Formula
C13H14N8O2
Formula Weight
314.3
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Ethanol: slightly solubleMethanol: slightly soluble
λmax
251, 286 nm
SMILES
O=C1C(N2C=CN=N2)=CNN1C3=NC=NC(N4CCOCC4)=C3
InChi Code
InChI=1S/C13H14N8O2/c22-13-10(20-2-1-16-18-20)8-17-21(13)12-7-11(14-9-15-12)19-3-5-23-6-4-19/h1-2,7-9,17H,3-6H2
InChi Key
IJMBOKOTALXLKS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    BAY 85-3934 is a pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases (HIF-PH; IC50s = 0.48, 0.28, and 0.45 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively).1 It stabilizes HIF-1α and HIF-2α levels in HeLa cells in a concentration- and time-dependent manner. BAY 85-3934 (50 µM) induces cell-cycle arrest at the G2/S phase in MDA-MB-231 breast cancer cells.2 It decreases lactate dehydrogenase (LDH) release from PC12 cells in an in vitro model of ischemia induced by oxygen-glucose deprivation when used at a concentration of 100 µM.3 BAY 85-3934 (5 mg/kg) increases plasma erythropoietin and hemoglobin levels, as well as packed cell volume, in a rat model of gentamicin-induced kidney failure.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Flamme, I., Oehme, F., Ellinghaus, P., et al. Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (molidustat) stimulates erythropoietin production without hypertensive effects. PLoS One 9(11), e111838 (2014).

    2. Kachamakova-Trojanowska , N., Podkalicka, P., Bogacz, T., et al. HIF-1 stabilization exerts anticancer effects in breast cancer cells in vitro and in vivo. Biochem. Pharmacol. 175, 113922 (2020).

    3. Singh, A., Wilson, J.W., Schofield, C.J., et al. Hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitors induce autophagy and have a protective effect in an in-vitro ischaemia model. Sci Rep. 10(1), 1597 (2020).

    Product Citations

    Wu, D., Su, X., Lu, J., et al. Bidirectional modulation of HIF-2 activity through chemical ligands. Nat. Chem. Biol. 15(4), 367-376 (2019).