TP0480066
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.
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- No. CAS: 2245693-15-4
- Fòrmula: C18H14FN3O5
- Peso molecular:371.32
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
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Topoisomerase II |
DNA gyrase 1.10 nM (IC50) |
topo IV 62.89 nM (IC50) |
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 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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)
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Concentration:0-2048 μg/mL
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Incubation Time:18-24 h
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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.
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Cell Line:N. gonorrhoeae ATCC (49226, 43069, BAA-1846, 700717, 700825), N. gonorrhoeae NCTC (13477, 13478, 13479, 13480, 13481, 13482, 13483, 13818, 13821)
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Concentration:0-2048 μg/mL
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Incubation Time:24-48 h
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Result:Exhibited significant antimicrobial activities to both N. gonorrhoeae and drug-resistant N. gonorrhoeae (MIC ranges both were ≤0.00012-0.0005 µg/mL)
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Cell Line:N. gonorrhoeae ATCC 49226
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Concentration:1.25×10-4, 5×10-4 and 2×10-3 µg/mL
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Incubation Time:24 h
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Result:Reduced the viable N. gonorrhoeae ATCC 49226 counts by more than 3-log10 CFU/mL (99.9%) after 6 h at 4× MIC and after 24 h at the MIC, respectively.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Slc:ICR mice[1]
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Dosage:100 mg/kg
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Administration:Subcutaneous injection, once.
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Result:
1.19 Pharmacokinetic Parameters of TP0480066 in Female Slc:ICR mice (n=3)[1].
Tmax (h) Cmax (ng/mL) AUC0-24 (ng/mL•h) 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]
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Dosage:1, 3, 10, 30 and 100 mg/kg
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Administration:Subcutaneous administration; single.
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Result:Significantly decreased mean viable cell counts of N. gonorrhoeae ATCC 49226 and NCTC 13479 when at 30, 100 mg/kg.
Chemical Information
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No. CAS 2245693-15-4
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Peso molecular 371.32
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Fòrmula C18H14FN3O5
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SMILES
CNC1=CC(F)=CC2=C1NC(C(C(NC3=CC=C(C=C3)C(O)=O)=O)=C2O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TP0480066 Related Classifications
HY-150045 Related Classifications
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