Fanotaprim (Synonyms: VYR-006)
目录号: PL03679 纯度: ≥98%
CAS No. :2120282-75-7
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中文名称
Fanotaprim
英文名称
Fanotaprim
英文别名
Fanotaprim;WJY2WD3C7A;Fanotaprim (USAN);Fanotaprim [USAN];5-{4-[3-(2-methoxypyrimidin-5-yl)phenyl]piperazin-1-yl}pyrimidine-2,4-diamine;5-(4-(3-(2-methoxypyrimidin-5-yl)phenyl)piperazin-1-yl)pyrimidine-2,4-diamine;5-[4-[3-(2-methoxypyrimidin-5-yl)phenyl]piperazin-1-yl]pyrimidine-2,4-diamine;BDBM50531784;TQ0154;WHO 11364;D11735;2,4-Pyrimidinediamine, 5-(4-(3-(2-methoxy-5-pyrimidiny
Cas No.
2120282-75-7
分子式
C19H22N8O
分子量
378.43
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Fanotaprim 是一种二氢叶酸还原酶 (DHFR) 抑制剂,对于 tgDHFR (Toxoplasma gondii DHFR) 和 hDHFR (human DHFR),IC50 分别为 1.57 和 308 nM。Fanotaprim 具有研究弓形虫病的潜力。
生物活性
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC 50 s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis.
性状
Solid
体外研究(In Vitro)
Fanotaprim shows parasiticidal and antiproliferative effects with EC50s of 13 and 7300 nM against the type I RH strain of T. gondii and MCF-7 cells, respectively.
Fanotaprim shows ability to inhibit the growth of T. gondii strains in vitro with EC50s ranging 7.6~ 29.8 nM (GT1, ME49, CTG, RUB and VAND). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Fanotaprim (1-10 mg/kg; p.o.; daily; beginning on day 1 through day 7) shows highly effective in control of acute infection by highly virulent strains of T. gondii in the murine model.
Fanotaprim (1mg/kg; i.v; mouse) shows C L , V d , and t 1/2 values of 10.6 mL/min/kg, 1.14 L/kg, and 3.9 hours, respectively.
Fanotaprim (0.83 mg/kg; p.o; mouse) shows F, C max , T max , and AUC 0-last of 47.3%, 178 ng/mL, 0.05 hours and 750 ng h/mL, respectively. 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
参考文献
[1]. Hopper AT, et al. Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis. J Med Chem. 2019;62(3):1562-1576.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (88.07 mM; ultrasonic and warming and heat to 60°C)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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