Brief Description

BAY-85-3934 is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells; HIF-stabilizer.
Target: HIF-stabilizer
in vitro: Under standard assay conditions, in the presence of 20 μM 2-oxoglutarate, 10 μM Fe2+, and 2 mM ascorbate, the mean IC50 values of BAY 85-3934 for PHD1, PHD2, and PHD3 were 480 nM, 280 nM, and 450 nM, respectively. Exposure of HeLa cells to 5 μM BAY 85-3934 for 20 min was sufficient to induce detectable concentrations of HIF-1α. In a cellular reporter assay, BAY 85-3934 induced the expression of the firefly luciferase reporter gene under the control of a hypoxia responsive element promoter at a mean (± SD) EC50 of 8.4± 0.7 μM (n=4) [1].
in vivo: EPO was significantly induced 7 h after administration of BAY 85-3934 (1.5 mg/kg) in all animals, and showed a clear increase after the 0.5 mg/kg dose in females [1].
References on BAY 85-3934:
[1]. Flamme I, et al. Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects. PLoS One. 2014 Nov 13;9(11):e111838.

Solubility

1 mg/ml in DMF(dimethyl formamide)

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Density

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Storage conditions

Store at -20°C 2 years

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