| Size | Price | Stock | Qty |
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| 1g |
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| 5g |
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| 10g |
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| 25g |
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| Other Sizes |
| Targets |
Octenidine dihydrochloride targets the microbial cell membrane. As a cationic surfactant, it interacts with the negatively charged components of the bacterial cell membrane, disrupting its integrity. This leads to leakage of cellular contents and rapid cell death. Unlike some other antiseptics, octenidine does not target specific proteins or enzymes but acts through a physical-chemical mechanism that is less prone to resistance development. Its activity against biofilms is mediated through the inhibition of biofilm gene expression, preventing the formation of these protective microbial communities. This broad-spectrum, non-specific mechanism makes it effective against a wide range of pathogens, including multidrug-resistant strains.
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| ln Vitro |
Concentrations of octenidine below 1.5 μM (0.94 μg/mL) resulted in a better than 99% reduction in the number of microorganisms tested after 15 minutes. Staphylococcus epidermidis was the most vulnerable of the bacteria examined, whereas Escherichia coli and Candida albicans were the least susceptible [1].
In vitro, Octenidine dihydrochloride demonstrates potent and rapid antimicrobial activity. Concentrations of less than 1.5 μM (0.94 μg/mL) cause a greater than 99% reduction of tested microbial populations within 15 minutes. It is active against a variety of bacteria, including methicillin-sensitive and -resistant Staphylococcus aureus. Its bactericidal activity is measured by exposing microbial cultures to various concentrations of the compound and determining the reduction in viable counts over time. The compound also inhibits biofilm formation. Its activity is not significantly affected by the presence of organic matter, making it suitable for use in wound care. |
| ln Vivo |
When examining the skin of cynomolgus monkeys' hands and feet, octenidine dihydrochloride (OCT) maintained its antibacterial action. The number of resident microbial communities is decreased from 90% to 99.98% by aqueous octenidine at a concentration of 0.2% to 1.6% [1]. On the lateral tooth surfaces of the face, a significant reduction in plaque scores was shown after topical application of 1% octinidine and chlorhexidine solution every day for 7 days; octinidine was more effective than chlorhexidine [2].
In vivo, Octenidine dihydrochloride demonstrates sustained antimicrobial activity upon application to the skin. Aqueous octenidine effectively diminishes resident microflora by 90 to 99.98% at concentrations ranging from 0.2 to 1.6%. It is used clinically as a topical antiseptic for skin, mucous membrane, and wound antisepsis. Its rapid and broad-spectrum activity, combined with good tissue tolerance, makes it a preferred agent for preventing and treating local infections. It is available as a 0.1-2.0% solution for various clinical applications. |
| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays are not applicable for Octenidine dihydrochloride, as it is a membrane-active agent rather than a specific enzyme inhibitor. Its antimicrobial activity is assessed through standard microbiological susceptibility tests. These include broth microdilution and agar diffusion methods to determine the minimum inhibitory concentration (MIC) against various bacterial and fungal strains. Time-kill assays are used to evaluate the kinetics of its bactericidal activity. Its ability to inhibit biofilm formation can be assessed using crystal violet staining or confocal microscopy.
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| Cell Assay |
In vitro cell-based assays for Octenidine dihydrochloride are used to evaluate its cytotoxicity and safety for topical applications. Mammalian cell lines, such as keratinocytes or fibroblasts, are treated with varying concentrations of the compound, and cell viability is measured using MTT or similar assays. These studies help to determine the therapeutic index of the compound, balancing its antimicrobial efficacy against its potential for tissue irritation. The compound's effects on wound healing can also be studied in cell culture models.
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| Animal Protocol |
In vivo animal studies for Octenidine dihydrochloride are conducted to evaluate its safety and efficacy in wound healing and infection models. The compound is applied topically to animal models with infected wounds or skin abrasions, and its effects on microbial load, wound healing rate, and tissue irritation are assessed. Standard protocols for skin irritation and sensitization are followed to ensure the compound's safety for clinical use. Its efficacy against specific pathogens, such as multidrug-resistant bacteria, can be evaluated in these models.
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| ADME/Pharmacokinetics |
Octenidine dihydrochloride has a molecular weight of 623.82 g/mol and a molecular formula of C₃₆H₆₂Cl₂N₄. It is a cationic surfactant and a bis-(dihydropyridinyl)-decane derivative. The compound is soluble in water and is typically formulated as a 0.1-2.0% aqueous solution for clinical use. It should be stored at room temperature, protected from light. Its stability in solution is good, making it suitable for various formulations.
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| Toxicity/Toxicokinetics |
Octenidine dihydrochloride has a favorable safety profile for topical use. It is well-tolerated on skin and mucous membranes, with low potential for irritation or sensitization. Systemic absorption is minimal, reducing the risk of systemic toxicity. It is not intended for oral or parenteral administration. In rare cases, allergic reactions may occur. The compound is considered safe for use in all age groups, including neonates.
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| References |
[1]. Sedlock DM, et al. Microbicidal activity of octenidine hydrochloride, a new alkanediylbis[pyridine] germicidal agent. Antimicrob Agents Chemother. 1985 Dec;28(6):786-90.
[2]. Emilson CG, et al. Effect of the antibacterial agents octenidine and chlorhexidine on the plaque flora in primates. Scand J Dent Res. 1981 Oct;89(5):384-92 |
| Additional Infomation |
Drug Indication
Skin disinfection; Treatment of upper respiratory tract infections; Prevention of oral soft tissue infections Octenidine dihydrochloride is a modern, broad-spectrum antiseptic used for skin, mucous membrane, and wound antisepsis. It is effective against multidrug-resistant pathogens and inhibits biofilm formation. It is a valuable alternative to other antiseptics like chlorhexidine and iodine. The compound is not a systemic drug and is intended for topical use only. It is approved for clinical use in many countries. |
| Molecular Formula |
C36H64CL2N4
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| Molecular Weight |
623.8262
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| Exact Mass |
622.45
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| CAS # |
70775-75-6
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| Related CAS # |
Octenidine;71251-02-0
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| PubChem CID |
51166
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| Appearance |
White to off-white solid powder
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| Boiling Point |
609.3ºC at 760 mmHg
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| Melting Point |
215-217ºC
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| Flash Point |
322.3ºC
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| LogP |
3.781
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
25
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| Heavy Atom Count |
42
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| Complexity |
691
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCC/N=C1C=CN(CCCCCCCCCCN(C=C/2)C=CC2=N/CCCCCCCC)C=C/1.Cl.Cl
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| InChi Key |
SMGTYJPMKXNQFY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C36H62N4.2ClH/c1-3-5-7-9-15-19-27-37-35-23-31-39(32-24-35)29-21-17-13-11-12-14-18-22-30-40-33-25-36(26-34-40)38-28-20-16-10-8-6-4-2;;/h23-26,31-34H,3-22,27-30H2,1-2H3;2*1H
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| Chemical Name |
N-octyl-1-[10-(4-octyliminopyridin-1-yl)decyl]pyridin-4-imine;dihydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~33.33 mg/mL (~53.43 mM)
DMSO : ~5 mg/mL (~8.02 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (4.01 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (4.01 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6030 mL | 8.0150 mL | 16.0300 mL | |
| 5 mM | 0.3206 mL | 1.6030 mL | 3.2060 mL | |
| 10 mM | 0.1603 mL | 0.8015 mL | 1.6030 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.