TP0480066

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Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
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Company Name: TargetMol Chemicals Inc.  
Tel: 13564774135
Email: marketing@targetmol.com

TP0480066 manufacturers

  • TP0480066
  • TP0480066 pictures
  • $1980.00
  • 2026-04-20
  • CAS:2245693-15-4
  • Purity:
  • Supply Ability: 10g
TP0480066 Basic information
Product Name:TP0480066
Synonyms:TP0480066
CAS:2245693-15-4
MF:C18H14FN3O5
MW:371.32
EINECS:
Product Categories:
Mol File:2245693-15-4.mol
TP0480066 Structure
TP0480066 Chemical Properties
Safety Information
MSDS Information
TP0480066 Usage And Synthesis
UsesTP0480066 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].
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 hng/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/mLh)t1/2 (h)
SC (100 mg/kg)0.25012400160006.79
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.
IC 50Topoisomerase II; DNA gyrase: 1.10 nM (IC50); topo IV: 62.89 nM (IC50)
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. DOI:10.1016/j.bmc.2020.115776
[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. DOI:10.1128/AAC.02145-20
TP0480066 Preparation Products And Raw materials
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