| Bioactivity | 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[1][2]. |
| Invitro | 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: |
| In Vivo | 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[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: |
| Name | TP0480066 |
| CAS | 2245693-15-4 |
| Formula | C18H14FN3O5 |
| Molar Mass | 371.32 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ushiyama F, et al. Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors. Bioorg Med Chem. 2020 Nov 15;28(22):115776. [2]. Masuko A, et al. In Vitro and In Vivo Activities of TP0480066, a Novel Topoisomerase Inhibitor, against Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2021 Mar 18;65(4):e02145-20. |
TP0480066
CAS: 2245693-15-4 F: C18H14FN3O5 W: 371.32
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respecti
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