产品
编 号：F750372
分子式：C18H14FN3O5
分子量：371.32
分子式：C18H14FN3O5
分子量：371.32
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CAS No: 2245693-15-4
产品详情
生物活性：
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea.
体内研究：
TP0480066 (100 mg/kg; s.c; once) demonstrates Cmax, Tmax, t1/2, and AUC0-24 h values of 12400 ng/mL, 0.250 h, 6.79 h, 16000 h?ng/mL, respectively.TP0480066 (1, 3, 10, 30, 100 mg/kg; s.c.; single) inhibits (30, 100 mg/kg) both N. gonorrhoeae ATCC 49226 and NCTC 13479 at 24 h and in a dose-dependent manner in mice.Animal Model:Female Slc:ICR mice
Dosage:100 mg/kg
Administration:Subcutaneous injection, once.
Result:1.19Pharmacokinetic Parameters of TP0480066 in Female Slc:ICR mice (n=3).Tmax (h)Cmax (ng/mL)AUC0-24 (ng/mL?h)t1/2 (h)
SC (100 mg/kg)0.25012400160006.79
Animal Model:Female BALB/c mice (6-week-old; genital tract infection model)
Dosage:1, 3, 10, 30 and 100 mg/kg
Administration:Subcutaneous administration; single.
Result:Significantly decreased mean viable cell counts of N. gonorrhoeae ATCC 49226 and NCTC 13479 when at 30, 100 mg/kg.
体外研究：
TP0480066 (compound 32) (0-2048 μg/mL; 18-24 h) demonstrats favorable antimicrobial activities against various bacterial species including some clinically isolated drug-resistant strains : MRSA (n=24), gPRSP (n=30), and VRE (n=34).TP0480066 (0-2048 μg/mL; 18-24 h) shows good antibacterial activity against Clostridioides difficile.TP0480066 (0-2048 μg/mL; 24-48 h) demonstrates potent antibacterial activity to N. gonorrhoeae, including strains with decreased susceptibility or resistance to currently available antimicrobial agents.TP0480066 (1.25×10-4, 5×10-4 and 2×10-3 μg/mL; 24 h) shows good time-kill activity when concentration up to (or more than) MIC (5×10-4 μg/mL) in N. gonorrhoeae ATCC 49226.
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea.
体内研究：
TP0480066 (100 mg/kg; s.c; once) demonstrates Cmax, Tmax, t1/2, and AUC0-24 h values of 12400 ng/mL, 0.250 h, 6.79 h, 16000 h?ng/mL, respectively.TP0480066 (1, 3, 10, 30, 100 mg/kg; s.c.; single) inhibits (30, 100 mg/kg) both N. gonorrhoeae ATCC 49226 and NCTC 13479 at 24 h and in a dose-dependent manner in mice.Animal Model:Female Slc:ICR mice
Dosage:100 mg/kg
Administration:Subcutaneous injection, once.
Result:1.19Pharmacokinetic Parameters of TP0480066 in Female Slc:ICR mice (n=3).Tmax (h)Cmax (ng/mL)AUC0-24 (ng/mL?h)t1/2 (h)
SC (100 mg/kg)0.25012400160006.79
Animal Model:Female BALB/c mice (6-week-old; genital tract infection model)
Dosage:1, 3, 10, 30 and 100 mg/kg
Administration:Subcutaneous administration; single.
Result:Significantly decreased mean viable cell counts of N. gonorrhoeae ATCC 49226 and NCTC 13479 when at 30, 100 mg/kg.
体外研究：
TP0480066 (compound 32) (0-2048 μg/mL; 18-24 h) demonstrats favorable antimicrobial activities against various bacterial species including some clinically isolated drug-resistant strains : MRSA (n=24), gPRSP (n=30), and VRE (n=34).TP0480066 (0-2048 μg/mL; 18-24 h) shows good antibacterial activity against Clostridioides difficile.TP0480066 (0-2048 μg/mL; 24-48 h) demonstrates potent antibacterial activity to N. gonorrhoeae, including strains with decreased susceptibility or resistance to currently available antimicrobial agents.TP0480066 (1.25×10-4, 5×10-4 and 2×10-3 μg/mL; 24 h) shows good time-kill activity when concentration up to (or more than) MIC (5×10-4 μg/mL) in N. gonorrhoeae ATCC 49226.
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