2. Cell Cycle/DNA Damage Anti-infection
  3. Topoisomerase Bacterial
  4. 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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TP0480066 Chemical Structure

TP0480066 Chemical Structure

CAS No. : 2245693-15-4

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TP0480066 Related Antibodies

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Description

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].

IC50 & Target

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.

TP0480066 Related Antibodies

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-log10 CFU/mL (99.9%) after 6 h at 4× MIC and after 24 h at the MIC, respectively.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Tmax (h) Cmax (ng/mL) AUC0-24 (ng/mL•h) t1/2 (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.
Molecular Weight

371.32

Formula

C18H14FN3O5
CAS No.
SMILES

CNC1=CC(F)=CC2=C1NC(C(C(NC3=CC=C(C=C3)C(O)=O)=O)=C2O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TP0480066 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TP04800662245693-15-4TP 0480066TP-0480066TopoisomeraseBacterialDNA gyraseantimicrobial resistanceAMRMRSAVRENeisseria gonorrhoeaeClostridioides difficileInhibitorinhibitorinhibit

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