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).
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.
分子式
C19H22N8O
分子量
378.43
CAS号
2120282-75-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.