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Molidustat

Chemical Structure : Molidustat

CAS No.: 1154028-82-6

Molidustat (BAY 85-3934;BAY 853934)

Catalog No.: PC-43140Not For Human Use, Lab Use Only.

Molidustat (BAY 85-3934) is an orally active small molecule inhibitor of hypoxia inducible factor prolyl hydroxylase (HIF-PHD) with IC50 of 480 nM, 280 nM and 450 nM for PHD1, PHD2, and PHD3, respectively.

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Biological Activity

Molidustat (BAY 85-3934) is an orally active small molecule inhibitor of hypoxia inducible factor prolyl hydroxylase (HIF-PHD) with IC50 of 480 nM, 280 nM and 450 nM for PHD1, PHD2, and PHD3, respectively.
Molidustat (BAY 85-3934) causes dose-dependent production of erythropoietin (EPO) in healthy Wistar rats and cynomolgus monkeys, increases hemoglobin levels and shows effectivity in the treatment of renal anemia in rats with impaired kidney function, resultsin normalization of hypertensive blood pressure in rat model of CKD.

Physicochemical Properties

M.Wt 314.3027
Formula C13H14N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: < 3.3 mg/mL

Chemical Name/SMILES

3H-Pyrazol-3-one, 1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)-

References

1. Flamme I, et al. PLoS One. 2014 Nov 13;9(11):e111838.

2. Beck H, et al. ChemMedChem. 2018 Feb 27. doi: 10.1002/cmdc.201700783.

3. Böttcher M, et al. Br J Clin Pharmacol. 2018 Mar 25. doi: 10.1111/bcp.13584.

4. Gupta N, et al. Am J Kidney Dis. 2017 Jun;69(6):815-826.

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