For research use only. Not for therapeutic Use.
Molidustat（Cat No.:I000565）, also known as BAY 85-3934, is a potent inhibitor of hypoxia-inducible factor proline hydroxylases (HIF-PHs). It exhibits inhibitory activity against PHD1, PHD2, and PHD3 enzymes with IC50 values of 480 nM, 280 nM, and 450 nM, respectively. By inhibiting HIF-PHs, solid-state stabilizes hypoxia-inducible factor (HIF) and increases the production of erythropoietin (EPO), which stimulates red blood cell production. Molidustat is being investigated for its potential use in the treatment of anemia associated with chronic kidney disease.
| Catalog Number | I000565 |
| CAS Number | 1154028-82-6 |
| Synonyms | 2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one |
| Molecular Formula | C₁₃H₁₄N₈O₂ |
| Purity | ≥95% |
| Target | HIF/HIF Prolyl-Hydroxylase |
| Solubility | DMSO: ＜ 3.3 mg/mL |
| Storage | Store at -20°C |
| IUPAC Name | 2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one |
| InChI | 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 |
| InChIKey | IJMBOKOTALXLKS-UHFFFAOYSA-N |
| SMILES | C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4 |
| Reference | </br>1:Mass spectrometric characterization of the hypoxia-inducible factor (HIF) stabilizer drug candidate BAY 85-3934 (molidustat) and its glucuronidated metabolite BAY-348, and their implementation into routine doping controls. Dib J, Mongongu C, Buisson C, Molina A, Schänzer W, Thuss U, Thevis M.Drug Test Anal. 2017 Jan;9(1):61-67. doi: 10.1002/dta.2011. Epub 2016 Jun 27. PMID: 27346747 </br>2:Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects. Flamme I, Oehme F, Ellinghaus P, Jeske M, Keldenich J, Thuss U.PLoS One. 2014 Nov 13;9(11):e111838. doi: 10.1371/journal.pone.0111838. eCollection 2014. PMID: 25392999 Free PMC Article |
