产品
编 号:F741377
分子式:C19H22N8O
分子量:378.43
产品类型
结构图
CAS No: 2120282-75-7
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产品详情
生物活性:
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s 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.
体内研究:
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.Animal Model:CD-1female mice (murine model of acute toxoplasmosis)
Dosage:1-10 mg/kg
Administration:p.o.; daily; beginning on day 1 through day 7
Result:Mice were monitored for survival for 30 days within termittent IVIS monitoring. At doses of 10 mg/kg Fanotaprim, q.d. or b.i.d. for 7 days, yielded 100% survival for 30 days.
体外研究:
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).