Abimufloxacin
Abimufloxacin (OPS-2071) is a broad-spectrum quinolone antibacterial agent. Abimufloxacin inhibits the supercoiling activity of DNA gyrase, the decatenation activity of topoisomerase IV, the activation and proliferation of T cells, macrophage activity, as well as the production of TNF-α and IFN-γ. Abimufloxacin exhibits activity against enteropathogenic Gram-positive bacteria, Gram-negative bacteria, quinolone-resistant bacteria, and Crohn's disease-associated bacteria (including Clostridioides difficile and Campylobacter jejuni). Abimufloxacin alleviates colonic inflammation in a mouse model of T cell-mediated colitis. Abimufloxacin can be used in research related to diseases such as intestinal infections and Crohn's disease.
For research use only. We do not sell to patients.
- CAS No.: 1426216-93-4
- Formula: C20H15FN4O3
- Molecular Weight:378.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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TNF-α |
DNA Gyrase |
TOPO IV |
Abimufloxacin (OPS-2071) exhibits potent broad-spectrum in vitro antibacterial activity against clinically isolated enteropathogenic Gram-positive bacteria (MSSA, MRSA, B. cereus) and Gram-negative bacteria (C. jejuni, E. coli, S. enterica, Shigella spp., Y. enterocolitica, A. hydrophila/sp., K. oxytoca, V. fluvialis, P. shigelloides). Compared with existing quinolone drugs, it shows stronger activity against MRSA and quinolone-resistant C. jejuni[1].
Abimufloxacin potently inhibits wild-type and quinolone-resistant mutant DNA gyrases of S. aureus and C. jejuni, while exhibiting comparable activity against E. coli DNA gyrase and topoisomerase IV[1].
Abimufloxacin (4‑64 × MIC; 18‑48 h) shows no detectable spontaneous resistance in Staphylococcus aureus ATCC 29231 and Escherichia coli ATCC 25922 at concentrations up to 64 × MIC; meanwhile, it confers a markedly lower spontaneous resistance rate for Campylobacter jejuni ATCC 33560 at 16 × MIC compared with existing quinolone drugs[1].
Abimufloxacin exhibits lower MPC against Staphylococcus aureus ATCC 29231 and Campylobacter jejuni ATCC 33560 than existing quinolone drugs, while its MPC against Escherichia coli ATCC 25922 is slightly higher than that of existing quinolone drugs, which indicates a lower risk of selecting drug‑resistant mutants in Gram‑positive bacteria and Campylobacter jejuni strains[1].
Abimufloxacin exhibits in vitro antibacterial activity against bacteria associated with inflammatory bowel disease (IBD), with an MICs range of 0.015 to 0.5 mg/mL[2].
Abimufloxacin (OPS-2071) inhibits TNF‑α production in human peripheral blood cells and THP‑1 macrophages in a dose‑dependent manner, suppresses the activation, proliferation and cytokine production of human peripheral blood mononuclear cells, and its effect at high concentrations is comparable to that of Prednisolone (HY‑17463)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1426216-93-4
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Molecular Weight 378.36
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Formula C20H15FN4O3
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SMILES
N#CC=1C=C(C=NC1N)C2=C(F)C=C3C(=O)C(=CN(C3=C2C)C4CC4)C(=O)O
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Synonyms
OPS-2071
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Abimufloxacin
- 1426216-93-4
- OPS-2071
- OPS2071
- OPS 2071
- Bacterial
- TNF Receptor
- Topoisomerase
- DNA/RNA Synthesis
- DNA gyrase
- THP-1 macrophages
- topoisomerase IV
- Clostridioides difficile
- murine T-cell-mediated colitis models
- Crohn’s disease
- Campylobacter jejuni
- Staphylococcus aureus
- human peripheral blood mononuclear cells
- Escherichia coli
- Inhibitor
- inhibitor
- inhibit