• 产品描述： Enarodustat (JTZ-951) 是一种有效的口服活性 HIF prolyl hydroxylase 抑制剂，对PHD2的IC50值为0.22 μM，对从Hep3B细胞释放EPO的EC50值为5.7 μM。Enarodustat 具有治疗肾性贫血的潜力

• 靶点： PHD2(Cell-free assay):0.22 μM; EPO release from Hep3B cells(Cell-based assay):5.7 μM(EC50);HIF/HIFProlyl-Hydroxylase

• 体内研究：
  JTZ-951 (compound 14), with a 5-phenethyl substituent on the triazolopyridine group, increases hemoglobin levels with daily oral dosing in rats. JTZ-951 is rapidly absorbed after oral administration and disappears shortly thereafter, which can be advantageous in terms of safety. JTZ-951 is selected as a clinical candidate.

• 细胞实验： Cell lines: Hep3B cells Concentrations: -- Incubation Time: 24 h Method: Human Hep3B cells are inoculated into 96-well flat-bottomed plates and on the next day, each test compound is added at appropriate concentrations for the assessment of EPO production. The culture supernatants are collected at 24 hours after the addition of each of the test compounds. A hypoxic condition is established and the EPO concentration of this condition is defined as 100% when the EC50 is calculated. The EPO concentration in culture supernatants is measured by human EPO ELISA kit.

• 动物实验： Animal Models: Male balb/c mice, CD (SD) rats Dosages: 1 mg/kg, 3 mg/kg Administration: Oral gavage

• 参考文献：
  1. Yosuke Ogoshi, et al. ACS Med Chem Lett. 2017 Nov 20;8(12):1320-1325.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.938 ml	14.692 ml	29.383 ml
  5 mM	0.588 ml	2.938 ml	5.877 ml
  10 mM	0.294 ml	1.469 ml	2.938 ml
  50 mM	0.059 ml	0.294 ml	0.588 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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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 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *