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Molidustat (BAY85-3934)Novel HIF-PH inhibitor

Molidustat (BAY85-3934)

Catalog No. B5861
Size Price Stock Qty
5mg $100.00 In stock
10mg $150.00 In stock
50mg $600.00 In stock
100mg $900.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Molidustat (BAY85-3934)

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Chemical Properties

Cas No. 1154028-82-6 SDF Download SDF
Chemical Name 2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one
Canonical SMILES O=C1C(N2C=CN=N2)=CNN1C3=NC=NC(N4CCOCC4)=C3
Formula C13H14N8O2 M.Wt 314.3
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Molidustat (BAY85-3934)

Description:

IC50: 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively.

Oxygen sensing via hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) is the dominant regulatory mechanism of erythropoietin (EPO) expression. In chronic kidney disease (CKD), impaired EPO expression causes anemia, which can be treated by supplementation with recombinant human EPO (rhEPO). Molidustat (BAY85-3934) is a novel HIF-PH inhibitor.

In vitro: The IC50 values were found to be dependent on the 2-oxoglutarate concentration in the reaction buffer. By lowering the 2-oxoglutarate concentration from 20 μM to 0.3 μM, the potency of the test compound increased up to 10-fold. Variation of the concentrations of Fe2+ and ascorbate in the reaction buffer by factors of 30 and 200, respectively, did not alter the potency of the inhibitor by more than 2-fold [1].

In vivo: In repeat dosing of BAY 85-3934, hemoglobin levels were increased compared with animals in vehicle group, while endogenous EPO remained within the normal physiological range. BAY 85-3934 therapy was also effective in the treatment of renal anemia in rats with impaired kidney function and, unlike treatment with rhEPO, resulted in normalization of hypertensive blood pressure in a rat model of CKD [1].

Clinical trial: Clinical studies are still ongoing to investigate the effects of BAY 85-3934 therapy in patients with renal anemia (https://clinicaltrials.gov/ct2/show/NCT01332942?term=Molidustat&rank=2).

Reference:
[1] Flamme I, Oehme F, Ellinghaus P, Jeske M, Keldenich J, Thuss U.  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.