| 中文名称: | Molidustat(BAY 853934) | ||||
|---|---|---|---|---|---|
| 英文名称: | Molidustat(BAY 853934) | ||||
| 别名: | 2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one | ||||
| CAS No: | 1154028-82-6 | 分子式: | C13H14N8O2 | 分子量: | 314.3 |
| CAS No: | 1154028-82-6 | ||||
| 分子式: | C13H14N8O2 | ||||
| 分子量: | 314.3 | ||||
| MDL: | MFCD28411428 | ||||
一种有效的缺氧诱导因子脯氨酸羟化酶(HIF-PH)抑制剂.IC50: 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively。
Oxygen sensing via hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) is the dominant regulatory mechanism of erythropoietin (EPO) expression. In chronic kidney disease (CKD), impaired EPO expression causes anemia, which can be treated by supplementation with recombinant human EPO (rhEPO). Molidustat is a novel HIF-PH inhibitor.
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 。
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。
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
