Molidustat is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells.
Under standard assay conditions, in the presence of 20 μM 2-oxoglutarate, 10 μM Fe2+, and 2 mM ascorbate, the mean IC50 values of BAY 85-3934 for PHD1, PHD2, and PHD3 were 480 nM, 280 nM, and 450 nM, respectively. Exposure of HeLa cells to 5 μM BAY 85-3934 for 20 min was sufficient to induce detectable concentrations of HIF-1α.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Flamme I, et al. 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.
分子式 C13H14N8O2 |
分子量 314.30 |
CAS号 1154028-82-6 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO Soluble |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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