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CAS No. : 2120282-75-7
MCE 国际站:Fanotaprim
产品活性: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。
研究领域:Cell Cycle/DNA Damage
作用靶点:Antifolate
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).
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 CL, Vd, and t1/2 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, Cmax, Tmax, and AUC0-last of 47.3%, 178 ng/mL, 0.05 hours and 750 ng h/mL, respectively.
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