化合物 TP0480066 T61481

Product Introduction
Bioactivity


英文名: 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

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途