TP0480066

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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.

For research use only. We do not sell to patients.

TP0480066 Chemical Structure

CAS No. : 2245693-15-4

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Topoisomerase Topo I Topo II

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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 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].

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].

	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.

Molecular Weight

371.32

Formula

C₁₈H₁₄FN₃O₅

CAS No.

2245693-15-4

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

Handling Instructions (2659 KB)

References

[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]

TP0480066 Related Classifications

Infection

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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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