2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. Molidustat sodium

Molidustat sodium 是一种具有口服活性的缺氧诱导因子脯氨酰羟化酶 (HIF-PH) 抑制剂，对 PHD1、PHD2 和 PHD3 的 IC50 值分别为 480 nM、 280 nM 和 450 nM。Molidustat sodium 可使循环中促红细胞生成素 (EPO) 水平升高至接近正常生理范围。Molidustat sodium 能用于肾性贫血的研究。

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Molidustat sodium Chemical Structure

Molidustat sodium Chemical Structure

CAS No. : 1375799-59-9

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Molidustat sodium 的其他形式现货产品:

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Molidustat sodium 相关抗体

Top Publications Citing Use of Products

查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Molidustat sodium 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 sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia[1][2].

IC50 & Target

IC50: 480 nM (PHD1), 280 nM (PHD2), 450 nM (PHD3)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 IC50
0.28 μM
Compound: 22; BAY-85-3934
Inhibition of recombinant human HIF-PHD2 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
Inhibition of recombinant human HIF-PHD2 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
10.1039/C6MD00240D
Sf9 IC50
0.45 μM
Compound: 22; BAY-85-3934
Inhibition of recombinant human HIF-PHD3 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
Inhibition of recombinant human HIF-PHD3 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
10.1039/C6MD00240D
Sf9 IC50
0.48 μM
Compound: 22; BAY-85-3934
Inhibition of recombinant human HIF-PHD1 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
Inhibition of recombinant human HIF-PHD1 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
10.1039/C6MD00240D
体外研究
(In Vitro)

Molidustat sodium (5 μM; 20 min) 在 HeLa 细胞中足以诱导可检测浓度的 HIF-1α。在细胞报告分析中，Molidustat sodium 在缺氧反应元件启动子的控制下诱导萤火虫荧光素酶报告基因的表达，平均 (± SD) EC50 为 8.4 μM (n=4)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molidustat sodium 相关抗体:
体内研究
(In Vivo)

Molidustat sodium (0.5-5 mg/kg; 口服; 一天一次连续 26 天) 在 Wistar 大鼠中 和 (0.5-1.5mg/kg; 一天一次连续 5 天) 食蟹猴中通过稳定缺氧诱导因子 (HIF) 导致健康 Wistar 大鼠和食蟹猴产生剂量依赖性的促红细胞生成素 (EPO)[1]。
Molidustat sodium (0.5-10 mg/kg; 口服; 每周五次) 可使慢性肾脏病 (CKD)大鼠模型中的高血压血压恢复正常，有效缓解肾功能受损大鼠的肾性贫血[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

336.28

Formula

C13H13N8NaO2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Molidustat sodium 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Molidustat1375799-59-9HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHrenal anemiaerythropoietin (EPO)HeLaWistar ratscynomolgus monkeyschronic kidney disease (CKD)Inhibitorinhibitorinhibit

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