2245693-15-4
2245693-15-4 structure
- Name: TP0480066
- Chemical Name: TP0480066
- CAS Number: 2245693-15-4
- Molecular Formula: C18H14FN3O5
- Molecular Weight: 371.32
- Catalog: Signaling Pathways Anti-infection Bacterial
- Create Date: 2022-09-16 19:40:31
- Modify Date: 2024-09-10 18:09:10
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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[1][2].
| Name | TP0480066 |
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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]. |
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| Related Catalog | |
| 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]. 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]. 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/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. |
| References |
| Molecular Formula | C18H14FN3O5 |
|---|---|
| Molecular Weight | 371.32 |