Enarodustat (Synonyms: JTZ-951; SAL0951)
目录号: PL11777 纯度: ≥99%
CAS No. :1262132-81-9
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中文名称
Enarodustat
英文名称
Enarodustat
英文别名
Enarodustat;JSK7TUA223;C17H16N4O4;Enarodustat [INN];Enarodustat (JAN);DB14985;J3.610.459G;D11523;(7-Hydroxy-5-phenethyl-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)glycine;Glycine, N-((7-hydroxy-5-(2-phenylethyl)(1,2,4)triazolo(1,5-a)pyridin-8-yl)carbonyl)-;N-[[7-Hydroxy-5-phenethyl-[1,2,4]triazolo[1,5-a]pyridine-8-yl]carbonyl]glycine
Cas No.
1262132-81-9
分子式
C17H16N4O4
分子量
340.33
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Enarodustat 是一种有效的,可口服的 hypoxia-inducible factor prolyl hydroxylase 抑制剂,EC50 of 0.22 μM。Enarodustat 有潜力用于肾性贫血症的研究。
生物活性
Enarodustat is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC 50 of 0.22 μM. Enarodustat has the potential for renal anemia treatment.
性状
Solid
IC50 & Target[1][2]
EC50: 0.22 μM (factor prolyl hydroxylase)
体外研究(In Vitro)
Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat exhibits neither CYP (IC50 > 100 μM; CYP3A4/5, CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2C19, CYP2C8, CYP2B6) nor hERG (IC50 > 100 μM) inhibition. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Ogoshi Y, et al. Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. ACS Med Chem Lett. 2017 Nov 20;8(12):1320-1325.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (244.85 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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