| 生物活性 | TP0480066 is a selectivetopoisomeraseIIinhibitor withIC50s of 1.10 and 62.89 nM forDNA gyraseandtopo IV, respectively. TP0480066 shows good activity of againsting variousbacterialspecies including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity toN. gonorrhoeae, can be used in study of gonorrhea[1][2]. |
| IC50& Target | Topoisomerase II | DNA gyrase 1.10 nM (IC50) | topo IV 62.89 nM (IC50) |
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体外研究
(In Vitro) | 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 againstClostridioides difficile[1].
TP0480066 (0-2048 μg/mL; 24-48 h) demonstrates potent antibacterial activity toN. gonorrhoeae, including strains with decreased susceptibility or resistance to currently available antimicrobial agents[2].
TP0480066 (1.25×10-4, 5×10-4and 2×10-3μg/mL; 24 h) shows good time-kill activity when concentration up to (or more than) MIC (5×10-4μg/mL) inN. gonorrhoeaeATCC 49226[2].
Cell Viability Assay[1] | Cell Line: | Clinically isolated Methicillin-resistantS. aureus(24 strains), Vancomycin-resistantenterococci(E. faecium(29 strains) andE. faecalis(5 strains), vanA positive (18 strains), vanB positive (14 strains) and vanA/vanB negative (2 strains)), Genotype penicillin-resistantS. 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. gonorrhoeaeATCC (49226, 43069, BAA-1846, 700717, 700825),N. gonorrhoeaeNCTC (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 bothN. gonorrhoeaeand drug-resistantN. gonorrhoeae(MIC ranges both were ≤0.00012-0.0005 μg/mL) |
Cell Viability Assay[2] | Cell Line: | N. gonorrhoeaeATCC 49226 | | Concentration: | 1.25×10-4, 5×10-4and 2×10-3μg/mL | | Incubation Time: | 24 h | | Result: | Reduced the viableN. gonorrhoeaeATCC 49226 counts by more than 3-log10CFU/mL (99.9%) after 6 h at 4× MIC and after 24 h at the MIC, respectively. |
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体内研究
(In Vivo) | TP0480066 (100 mg/kg; s.c; once) demonstrates Cmax, Tmax, t1/2, and AUC0-24 hvalues of 12400 ng/mL, 0.250 h, 6.79 h, 16000 hong/mL, respectively[2].
TP0480066 (1, 3, 10, 30, 100 mg/kg; s.c.; single) inhibits (30, 100 mg/kg) bothN. gonorrhoeaeATCC 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: | 1.19Pharmacokinetic Parameters of TP0480066 in Female Slc:ICR mice (n=3)[1].
| Tmax(h) | Cmax(ng/mL) | AUC0-24(ng/mLoh) | t1/2(h) | | SC (100 mg/kg) | 0.250 | 12400 | 16000 | 6.79 |
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| 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 ofN. gonorrhoeaeATCC 49226 and NCTC 13479 when at 30, 100 mg/kg. |
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| 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. |
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