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| Targets |
Quinolone
Norfloxacin hydrochloride primarily targets bacterial enzymes, specifically DNA gyrase and topoisomerase IV. These enzymes are crucial for bacterial DNA replication, transcription, repair, and recombination. By inhibiting these enzymes, norfloxacin hydrochloride disrupts the bacterial DNA processes, leading to the death of the bacteria. The compound has a 100 times higher affinity for bacterial DNA gyrase than for mammalian. Its mode of action involves blocking bacterial DNA replication by binding to the enzyme DNA gyrase, which prevents the untwisting required to replicate one DNA double helix into two. Norfloxacin hydrochloride affects the biochemical pathways involved in bacterial DNA replication and transcription. By inhibiting DNA gyrase and topoisomerase IV, the compound disrupts these pathways, leading to the cessation of bacterial growth and multiplication. |
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| ln Vitro |
A synthetic chemotherapeutic antibacterial drug called norfloxacin (MK-0366) is sporadically used to treat both simple and complex urinary tract infections. A broad-spectrum antibiotic that works against both Gram-positive and Gram-negative bacteria is norfloxacin (MK-0366). It works by blocking the enzymes DNA gyrase, a type II topoisomerase, and topoisomerase IV, which are required to separate the DNA of bacteria and prevent cell division. In the adult population, there are presently three approved uses (one restricted), and the other is ineffective because of bacterial resistance.
In vitro, norfloxacin hydrochloride exhibits broad-spectrum bactericidal activity against Gram-negative and some Gram-positive pathogens. It is used as a model compound in the study of fluoroquinolone antibiotics and their chemical properties. The compound is used in microbiological studies to investigate the mechanisms of bacterial resistance and the effects of antibiotics on bacterial cells. Its activity is concentration-dependent, with higher concentrations leading to more rapid bacterial killing. The compound's ability to inhibit DNA gyrase and topoisomerase IV makes it effective against a wide range of bacterial species, including those resistant to other classes of antibiotics. |
| ln Vivo |
In vivo, norfloxacin hydrochloride is extensively studied for its therapeutic applications in treating bacterial infections. It is used in clinical trials to evaluate its efficacy and safety in various patient populations. The drug is effective against urinary tract infections, gastrointestinal infections, and other bacterial infections caused by susceptible organisms. Following oral administration, approximately 30 to 40% of the compound is rapidly absorbed. Peak serum concentrations of 1.5 to 2.0 pg/ml are achieved within one to two hours after a 400-mg dose. The drug is widely distributed throughout the body and undergoes hepatic metabolism. Approximately 30% of an administered dose is excreted as unchanged drug by glomerular filtration and tubular secretion.
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| Enzyme Assay |
In vitro non-cell enzyme assays for norfloxacin hydrochloride typically involve measuring the inhibition of DNA gyrase and topoisomerase IV activity using purified enzymes. The compound is incubated with the enzyme and a DNA substrate, and the extent of DNA supercoiling or relaxation is measured by gel electrophoresis or fluorescence-based assays. IC₅₀ values are calculated from dose-response curves. The compound's binding affinity to its targets can be assessed using surface plasmon resonance or isothermal titration calorimetry. These assays provide quantitative data on the compound's direct interactions with its molecular targets.
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| Cell Assay |
In vitro cell-based assays for norfloxacin hydrochloride use various bacterial strains to determine minimum inhibitory concentrations (MIC) using broth microdilution or agar diffusion methods according to CLSI guidelines. The compound is tested against a panel of Gram-negative and Gram-positive pathogens to evaluate its spectrum of activity. Time-kill assays are performed to assess the bactericidal activity of the compound over time. Resistance development studies are conducted by serial passaging of bacteria in the presence of sub-inhibitory concentrations of the compound. Cytotoxicity assays using mammalian cell lines are performed to evaluate the compound's selectivity for bacterial targets.
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| Animal Protocol |
In vivo animal studies for norfloxacin hydrochloride employ rodent models of bacterial infection, such as urinary tract infection or sepsis models. The compound is administered orally or intravenously, and parameters such as bacterial clearance from blood and tissues, survival rates, and reduction of infection symptoms are assessed. Pharmacokinetic studies in these models provide information about the compound's absorption, distribution, metabolism, and excretion. Tissue distribution studies evaluate the compound's penetration into target tissues such as the kidneys and prostate. Toxicological studies assess the compound's safety profile, including potential effects on the gastrointestinal tract, kidneys, and central nervous system.
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| ADME/Pharmacokinetics |
Norfloxacin hydrochloride has a molecular weight of 355.79 g/mol and a molecular formula of C₁₆H₁₈FN₃O₃·HCl. Following oral administration, approximately 30 to 40% of the compound is rapidly absorbed. Peak serum concentrations of 1.5 to 2.0 pg/ml are achieved within one to two hours after a 400-mg dose. The drug is widely distributed throughout the body and undergoes hepatic metabolism. Approximately 30% of an administered dose is excreted as unchanged drug by glomerular filtration and tubular secretion. The compound has a terminal elimination half-life of approximately three hours. It has good penetration into kidney and prostatic tissues.
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| Toxicity/Toxicokinetics |
The toxicity profile of norfloxacin hydrochloride includes gastrointestinal disturbances, such as nausea, vomiting, and diarrhea, which are common side effects of fluoroquinolone antibiotics. Central nervous system effects, including dizziness, headache, and confusion, may occur. The compound can cause tendonitis and tendon rupture, particularly in older patients or those on corticosteroid therapy. Photosensitivity reactions may occur with exposure to sunlight or UV radiation. The compound is contraindicated in patients with a history of hypersensitivity to fluoroquinolones. As a research compound, norfloxacin hydrochloride is not intended for human therapeutic use without appropriate regulatory approval. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Norfloxacin hydrochloride is a second-generation fluoroquinolone antibiotic that functions as a DNA gyrase and topoisomerase IV inhibitor. It exhibits broad-spectrum bactericidal activity against Gram-negative and some Gram-positive pathogens. The compound is extensively studied for its therapeutic applications in treating bacterial infections. Following oral administration, approximately 30 to 40% of the compound is rapidly absorbed. Peak serum concentrations of 1.5 to 2.0 pg/ml are achieved within one to two hours after a 400-mg dose. The drug is widely distributed throughout the body and undergoes hepatic metabolism. Approximately 30% of an administered dose is excreted as unchanged drug by glomerular filtration and tubular secretion. The compound has a terminal elimination half-life of approximately three hours. It is used as a model compound in the study of fluoroquinolone antibiotics. Not approved for human therapeutic use without appropriate regulatory approval.
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| Molecular Formula |
C16H19CLFN3O3
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|---|---|
| Molecular Weight |
355.109894
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| Exact Mass |
355.11
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| Elemental Analysis |
C, 54.01; H, 5.38; Cl, 9.96; F, 5.34; N, 11.81; O, 13.49
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| CAS # |
68077-27-0
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| Related CAS # |
Norfloxacin;70458-96-7
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| PubChem CID |
12733888
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| Appearance |
Solid powder
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| LogP |
1.662
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
519
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CN(CC)C2=C(C=C(F)C(N3CCNCC3)=C2)C1=O)O.Cl
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| InChi Key |
JJWDELPVPRCLQN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18FN3O3.ClH/c1-2-19-9-11(16(22)23)15(21)10-7-12(17)14(8-13(10)19)20-5-3-18-4-6-20;/h7-9,18H,2-6H2,1H3,(H,22,23);1H
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| Chemical Name |
1-ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride
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| Synonyms |
Norfloxacin hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8160 mL | 14.0801 mL | 28.1603 mL | |
| 5 mM | 0.5632 mL | 2.8160 mL | 5.6321 mL | |
| 10 mM | 0.2816 mL | 1.4080 mL | 2.8160 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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