| 名称 | TP0480066 |
| 描述 | TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2]. |
| 体外活性 | 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) [1]. TP0480066 (0-2048 μg/mL; 18-24 h) shows good antibacterial activity against Clostridioides difficile [1]. 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 [2]. 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 [2]. Cell Viability Assay [1] Cell Line: Clinically isolated Methicillin-resistant S. aureus (24 strains), Vancomycin-resistant enterococci ( E. faecium (29 strains) and E. faecalis (5 strains), vanA positive (18 strains), vanB positive (14 strains) and vanA/vanB negative (2 strains)), Genotype penicillin-resistant S. pneumonia (30 strains) Concentration: 0-2048 μg/mL Incubation Time: 18-24 h Result: Showed favorable antimicrobial activities to drug-resistant strains with MIC ranges of 0.03-0.5, 0.015-0.25 and 0.002-0.015 μg/mL for MRSA (n=24), gPRSP (n=30), and VRE (n=34), respectively. Cell Viability Assay [2] Cell Line: N. gonorrhoeae ATCC (49226, 43069, BAA-1846, 700717, 700825), N. gonorrhoeae NCTC (13477, 13478, 13479, 13480, 13481, 13482, 13483, 13818, 13821) Concentration: 0-2048 μg/mL Incubation Time: 24-48 h Result: Exhibited significant antimicrobial activities to both N. gonorrhoeae and drug-resistant N. gonorrhoeae (MIC ranges both were ≤0.00012-0.0005 μg/mL) Cell Viability Assay [2] Cell Line: N. gonorrhoeae ATCC 49226 Concentration: 1.25×10 -4, 5×10 -4 and 2×10 -3 μg/mL Incubation Time: 24 h Result: Reduced the viable N. gonorrhoeae ATCC 49226 counts by more than 3-log 10 CFU/mL (99.9%) after 6 h at 4× MIC and after 24 h at the MIC, respectively. |
| 体内活性 | TP0480066 (100 mg/kg; s.c; once) demonstrates C max, T max, t 1/2, and AUC 0-24 h values of 12400 ng/mL, 0.250 h, 6.79 h, 16000 h ng/mL, respectively [2]. 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 [2]. Animal Model: Female Slc:ICR mice [1] Dosage: 100 mg/kg Administration: Subcutaneous injection, once. Result: 1.19 Pharmacokinetic Parameters of TP0480066 in Female Slc:ICR mice (n=3) [1]. T max (h) C max (ng/mL) AUC 0-24 (ng/mL h) t 1/2 (h) SC (100 mg/kg) 0.250 12400 16000 6.79 Animal Model: Female BALB/c mice (6-week-old; genital tract infection model) [2] 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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