- Molidustat ;BAY85-3934
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- $0.00 / 1g
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2024-11-01
- CAS:1154028-82-6
- Min. Order: 1g
- Purity: 98%
- Supply Ability: 100kgs
- Molidustat
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- $1.00 / 1KG
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2019-12-24
- CAS:1154028-82-6
- Min. Order: 1KG
- Purity: Min98% HPLC
- Supply Ability: g/kg/ton
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| | Molidustat(BAY 85-3934) Basic information |
| Product Name: | Molidustat(BAY 85-3934) | | Synonyms: | Molidustat(BAY 85-3934);BAY 85-3934;MOLIDUSTAT;2-[6-(4-Morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one;2-[6-(Morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one;Somatoprim;2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one;1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)-3H-pyrazol-3-one | | CAS: | 1154028-82-6 | | MF: | C13H14N8O2 | | MW: | 314.3 | | EINECS: | 815-038-0 | | Product Categories: | Inhibitors;API | | Mol File: | 1154028-82-6.mol |  |
| | Molidustat(BAY 85-3934) Chemical Properties |
| 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 |
| | Molidustat(BAY 85-3934) Usage And Synthesis |
| Description | Hypoxia-inducible factor (HIF) is the major transcription factor involved in erythropoietin gene expression. Because oxygen-dependent degradation of the α subunit of HIF suppresses erythropoietin expression, stimulation of erythropoiesis by agents that prevent degradation of HIF has been one strategy for managing anemia. BAY 85-3934 stabilizes HIF from degradation in the proteasome by inhibiting HIF-1α prolyl hydroxylase (IC50 = 0.49 μM). Inhibition of HIF prolyl hydroxylase by BAY 85-3934 has been shown to increase endogenous production of erythropoietin. This compound has been investigated in clinical trial for treatment of patients with anemia associated with chronic kidney disease and/or end-stage renal disease. | | 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 |
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