Molidustat(BAY 85-3934)
- CAS No.
- 1154028-82-6
- Chemical Name:
- Molidustat(BAY 85-3934)
- Synonyms
- MOLIDUSTAT;CS-1728;Somatoprim;BAY 85-3934;Molidustat(BAY 85-3934);BAY 85-3934;BAY-85-3934;2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one;2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one;2-(6-morpholinopyrimidin-4-yl)-4-(1h-1,2,3-triazol-1-yl)-1,2-dihydro-3h-pyrazol-3-one;1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)-3H-pyrazol-3-one
- CBNumber:
- CB72729607
- Molecular Formula:
- C13H14N8O2
- Molecular Weight:
- 314.3
- MDL Number:
- MFCD28411428
- MOL File:
- 1154028-82-6.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Boiling point | 589.2±60.0 °C(Predicted) |
|---|---|
| Density | 1.67±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | insoluble in EtOH; insoluble in H2O; ≥5.68 mg/mL in DMF |
| form | solid |
| pka | 5.38±0.37(Predicted) |
| color | White to off-white |
| 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 | N1C=C(N2C=CN=N2)C(=O)N1C1C=C(N2CCOCC2)N=CN=1 |
| FDA UNII | 9JH486CZ13 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS08,GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H372-H360-H302 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501-P260-P264-P270-P314-P501 | |||||||||
| NFPA 704 |
|
Molidustat(BAY 85-3934) price More Price(48)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 15297 | BAY 85-3934 ≥95% | 1154028-82-6 | 1mg | $37 | 2026-04-30 | Buy |
| Cayman Chemical | 15297 | BAY 85-3934 ≥95% | 1154028-82-6 | 5mg | $151 | 2026-04-30 | Buy |
| Cayman Chemical | 15297 | BAY 85-3934 ≥95% | 1154028-82-6 | 10mg | $246 | 2026-04-30 | Buy |
| Cayman Chemical | 15297 | BAY 85-3934 ≥95% | 1154028-82-6 | 25mg | $436 | 2026-04-30 | Buy |
| Biosynth | EWB02882 | Molidustat | 1154028-82-6 | 0.05g | $171.88 | 2026-06-04 | Buy |
Molidustat(BAY 85-3934) Chemical Properties, Uses, Production
Description
Hypoxia-inducible factor (HIF) is the major transcription factor involved in erythropoietin gene expression. Because oxygen-
Uses
Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia[1][2].
Synthesis
5767-36-2
1021869-28-2
1154028-82-6
Example 23: 10.0 g (51.2 mmol) of 4-(6-hydrazinopyrimidin-4-yl)morpholine and 10.7 g (53.8 mmol) of 3-(dimethylamino)-2-(1H-1 ,2,3-triazol-1-yl)methyl acrylate were suspended in 100 mL of n-butyl acetate, 2.92 g (25.6 mmol) of trifluoroacetic acid was added, and the reaction was carried out at reflux temperature (about 120 °C) and the reaction was stirred for 6 hours. Upon completion of the reaction, the reaction mixture was cooled to 20 °C and stirring was continued for 16 h, followed by stirring at 0 °C for 1 h and filtration. The resulting solid was washed twice with cold ethyl acetate (4 mL each time) and dried under reduced pressure at 40 °C. The solid (15.5 mL) was then washed with cold ethyl acetate. The dried solid (15.6 g) was suspended in 100 mL of water, 2.4 mL of acetic acid was added and stirred at 50 °C for 30 min. After cooling to 20 °C, the suspension was filtered, the solid was washed twice with water (10 mL each time) and dried under reduced pressure at 40 °C to afford 13.9 g of the target product, 2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one, in 86.3% (as theoretical) yield and 99.7 purity Area%, and 99.0 wt%.
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].
IC 50
480 nm, 280 nm, and 450 nm for phd1, phd2, and phd3, respectively.
References
[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.
Molidustat(BAY 85-3934) Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Chengdu Yuyang High-tech Development Co., Ltd. | 02861777709 13308012069 | 13308012069@189.cn | China | 39 | 58 |
| Nanjing Paite Meisheng Technology Co., Ltd | 15952038335 13327728092 | xu_meiqin@petmedtech.com | China | 30 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2915 | 55 | |
| Energy Chemical | 400-0056266 | sales8178@energy-chemical.com | China | 44850 | 61 |
| Shanghai Hanhong Scientific Co.,Ltd. | 021-54306202 13764082696 | info@hanhongsci.com | China | 42917 | 64 |
| Artis Chemistry (Shanghai) Co. Ltd. | 86-21-60936353 | China | 335 | 58 | |
| Shanghai Topbiochem Technology Co., Ltd | 021-58170097 | info@topbiochem.com | China | 9509 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| Guangzhou Isun Pharmaceutical Co., Ltd | 020-39119399 18927568969 | isunpharm@qq.com | China | 4773 | 55 |
| CEG Chemical Science&Technology Co., Ltd. | Mobile:13665161512 | China | 1784 | 58 |
View Latest Price from Molidustat(BAY 85-3934) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-01 | Molidustat ;BAY85-3934
1154028-82-6
|
1g | 98% | 100kgs | Wuhan Nutra Biotechnology Co.,Ltd | ||
 |
2019-12-24 | Molidustat
1154028-82-6
|
$1.00 | 1KG | Min98% HPLC | Career Henan Chemical Co |
-
- Molidustat ;BAY85-3934
1154028-82-6
- 98%
- Wuhan Nutra Biotechnology Co.,Ltd
-
- Molidustat
1154028-82-6
- $1.00
- Min98% HPLC
- Career Henan Chemical Co
