research use only
Cat.No.S1940
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Other Topoisomerase Inhibitors | Camptothecin (CPT) Betulinic acid Beta-Lapachone (S)-10-Hydroxycamptothecin Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Cu(II)-Elesclomol Hydroxy Camptothecine Rubitecan |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| HEK293 cells | Function assay | 1.5 mins | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=17.9 μM | |||
| human 5637 cells | Function assay | 200 to 300 ug/ml | 12 h | Antibacterial activity against uropathogenic Escherichia coli UTI89 infected in human 5637 cells assessed as decrease in intracellular bacterial level at 200 to 300 ug/ml after 12 hrs by serial dilution method | ||
| Click to View More Cell Line Experimental Data | ||||||
| Molecular Weight | 361.37 | Formula | C18H20FN3O4 |
Storage (From the date of receipt) | |
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| CAS No. | 100986-85-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | Fluoroquinolone | Smiles | CC1COC2=C3N1C=C(C(=O)C3=CC(=C2N4CCN(CC4)C)F)C(=O)O | ||
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In vitro |
DMSO
: 18 mg/mL
(49.81 mM)
Water : 18 mg/mL Ethanol : 2 mg/mL |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Targets/IC50/Ki |
Topoisomerase II
Topoisomerase IV
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|---|---|
| In vitro |
Levofloxacin is active against most aerobic Gram-positive and Gram-negative organisms and demonstrates moderate activity against anaerobes. This compound is two-fold more active than ciprofloxacin against Streptococcus pneumoniae and 2- to 4-fold more active than ciprofloxacin against Staphylococcus aureus, Xanthomonas maltophilia, and Bacteroides fragilis. It is two- to eightfold more active than ciprofloxacin against coagulase-negative staphylococci and Acinetobacter spp., although these improvements in potency may not be clinically relevant. This agent inhibits 90% of streptococci when it is used at concentrations of 1 mg/mL to 2 mg/mL. It exhibits twofold greater inhibitory and bactericidal activities than ofloxacin against either extracellular or intracellular tubercle bacilli. This compound has the least inhibitory effect on osteoblastic cell growth, with a 50% inhibitory concentration of approximately 80 mg/mL at 48 and 72 hours. It results in strong inhibition of calcium deposition, as determined on day 14 by alizarin red staining and biochemical analysis. It inhibits glycosaminoglycan synthesis initially and DNA synthesis and mitochondrial function secondarily at actual arthropathic concentrations in cultured rabbit chondrocytes but that these changes are reversible and not enough to kill the cells.
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| In vivo |
Levofloxacin is as efficacious as or more efficacious than that with ciprofloxacin in systemic as well as pyelonephritis infections in mice. This compound achieves higher concentrations in the serum and tissue of mice than does ciprofloxacin.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05743101 | Not yet recruiting | Acute Ischemic Stroke |
Yi Yang|The First Hospital of Jilin University |
April 1 2024 | Not Applicable |
| NCT05799326 | Recruiting | Acute Ischemic Stroke |
Yi Yang|The First Hospital of Jilin University |
June 30 2023 | Not Applicable |
| NCT05741905 | Recruiting | Acute Ischemic Stroke |
Yi Yang|The First Hospital of Jilin University |
June 1 2023 | Not Applicable |
| NCT05441930 | Withdrawn | Cataract |
PolyActiva Pty Ltd |
June 23 2023 | Phase 1 |
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