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Desidustat

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Chemical Structure| 1616690-16-4 同义名 : ZYAN1;Taleranol;Desidustat, ZYan1;β-Zearanol;β-Zearalanol;P 1560;ZYAN1-1001
CAS号 : 1616690-16-4
货号 : A724200
分子式 : C16H16N2O6
纯度 : 99%+
分子量 : 332.31
MDL号 : MFCD31630836
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(27.08 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Desidustat is a pan-PHD (prolyl hydroxylase) inhibitor used for the treatment of chronic kidney disease-induced anemia, acting by inducing erythropoiesis by stabilizing hypoxia-inducible factor (HIF). A single dose treatment of 15mg/kg Desidustat attenuated the effect of LPS or turpentine oil-induced inflammation and increased serum erythropoietin, iron, and reticulocyte count, and decreased serum hepcidin levels. Repeated treatment of Desidustat at dose ranging in 5-50mg/kg increased hemoglobin, RBC and hematocrit in a dose related manner in turpentine oil-induced anemia in BALB/c mice. Desidustat at dose of 15mg/kg and 30mg/kg markedly reduced PGPS-induced anemia and increased hemoglobin, RBC and WBC count, hematocrit, serum iron and spleen iron in female Lewis rats. Meanwhile, it caused a significant increase in expression of DcytB, FPN1, DMT1, MCP-1 in liver, suggesting an overall influence on iron metabolism.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.05mL

3.01mL

1.50mL

30.09mL

6.02mL

3.01mL
参考文献

[1]Joharapurkar AA, Pandya VB, et al. Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. J Med Chem. 2018 Aug 23;61(16):6964-6982.

[2]Patel H, Joharapurkar AA, et al. Influence of acute and chronic kidney failure in rats on the disposition and pharmacokinetics of ZYAN1, a novel prolyl hydroxylase inhibitor, for the treatment of chronic kidney disease-induced anemia. Xenobiotica. 2018 Jan;48(1):37-44.

[3]Jain M, Joharapurkar A, et al. Pharmacological inhibition of prolyl hydroxylase protects against inflammation-induced anemia via efficient erythropoiesis and hepcidin downregulation. Eur J Pharmacol. 2019 Jan 15;843:113-120.