| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Targets |
Chloroxine's mechanism of action is not fully understood. As an 8-hydroxyquinoline derivative, it likely chelates metal ions essential for microbial enzymes, disrupting essential metabolic processes. It exhibits antibacterial, antifungal, antiprotozoal, and antiamoebic activities. It is effective against a broad range of microorganisms.
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| ln Vitro |
The chlorine-oxygen solubility demonstrated a strong association when the Jouyban-Acree model was applied, yielding RAD values below 3.64% and RMSD values below 8.82 × 10−6. Chloroxine was preferentially solvated by DMSO (DMF, NMP, or 1,4-dioxin) in compositions that were intermediate and cosolvent-rich, but chloroxygen was preferentially solvated by water for the mixes under study in compositions that were water-rich. Mixtures of DMSO (DMF, NMP, or 1,4-dioxane) + water are used to solvate alkanes. The findings indicate that the hole term's effects on the solvent-solvent interaction energy regulate how soluble oxychloroxane becomes in all aqueous mixtures [1].
In vitro, chloroxine demonstrates effective antibacterial, antifungal, antiprotozoal, and antiamoebic activities. It is effective against various pathogens, including those causing dandruff and seborrheic dermatitis. Specific MIC values against various organisms are documented in the literature but not detailed in the available results. |
| ln Vivo |
In vivo, chloroxine is used clinically for the treatment of dandruff and mild to moderately severe seborrheic dermatitis when incorporated in a shampoo. It is also used for the treatment of intestinal amebiasis. It is effective as a topical and intestinal antimicrobial agent.
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| Enzyme Assay |
In vitro antimicrobial susceptibility testing is performed using broth microdilution or agar dilution methods. Chloroxine is tested at various concentrations against bacterial, fungal, and protozoal cultures. MIC values are determined after appropriate incubation periods. Chelation studies may assess metal ion binding.
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| Cell Assay |
In vitro cell-based assays for antimicrobial activity use various microbial cultures (e.g., bacteria, fungi, protozoa). Cells are treated with chloroxine at various concentrations, and growth inhibition is assessed spectrophotometrically or by colony counting. Antiamoebic activity is assessed using Entamoeba histolytica cultures.
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| Animal Protocol |
In vivo efficacy for seborrheic dermatitis and dandruff is evaluated in human clinical trials, where chloroxine-containing shampoos are applied topically. Endpoints include reduction in scaling, itching, and erythema. For intestinal amebiasis, efficacy is evaluated in patients with confirmed infection. Animal models of infection may also be used.
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| ADME/Pharmacokinetics |
Chloroxine is a synthetic quinoline derivative. As a topical agent in shampoos, systemic absorption is limited. When used for intestinal amebiasis, it is administered orally and has some systemic absorption. Specific pharmacokinetic parameters are not extensively documented in the available literature. It is excreted in urine and feces.
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| Toxicity/Toxicokinetics |
Chloroxine is generally well-tolerated topically. Local skin irritation or allergic reactions may occur. When used orally for amebiasis, gastrointestinal disturbances may occur. Systemic toxicity is rare at therapeutic doses. It should be used with caution in patients with known hypersensitivity to 8-hydroxyquinoline derivatives.
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| References |
[1]. Renjie X, et al. Solubility modelling, solvent effect and preferential solvation of carbendazim in aqueous co-solvent mixtures of, N,N -dimethylformamide, methanol, ethanol and, n -propanol. J. Chem. Thermodynamics 138 (2019) 288–296.
[2]. Chloroxine (Topical). Dec 27, 2018 |
| Additional Infomation |
Chloroxine is a monohydroxyquinoline, a derivative of quinoline-8-ol, in which the hydrogen atoms at positions 5 and 7 are replaced by chlorine atoms. It is a synthetic antibacterial agent prepared by chlorination of quinoline-8-ol and used to treat dandruff and seborrheic dermatitis. It has antibacterial, anti-seborrheic, and antifungal effects. It is a monohydroxyquinoline and organochlorine compound whose structure is related to quinoline-8-ol. Chloroxine is a synthetic antibacterial compound. Chloroxine is one of the ingredients in some shampoos used to treat dandruff and seborrheic dermatitis. Chloroxine is a synthetic quinoline derivative with antibacterial activity. Although its mechanism of action is not fully elucidated, topical application of Chloroxine can reduce the mitotic activity of epidermal cells, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis (including psoriasis and eczema). Drug Indications: For the treatment of dandruff and mild to moderate seborrheic dermatitis. Mechanism of Action While its mechanism of action is not fully elucidated, Chloroxine may slow the mitotic activity of epidermal cells, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis. Chloroxineyquine can induce SOS-DNA repair in Escherichia coli, therefore it may have genotoxic effects on bacteria. Pharmacodynamics Chloroxineyquine has antibacterial activity, inhibiting the growth of Gram-positive bacteria and some Gram-negative bacteria. Furthermore, Chloroxine also shows antifungal activity against certain dermatophytes and yeasts.
Chloroxine (5,7-Dichloro-8-quinolinol) is a synthetic antibacterial and antifungal agent used in the treatment of dandruff and seborrheic dermatitis. It is also used for intestinal amebiasis. It is available in over-the-counter and prescription shampoos and as an oral medication in some countries. Its use has decreased with the availability of newer antifungal agents. |
| Molecular Formula |
C9H5CL2NO
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|---|---|
| Molecular Weight |
214.05
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| Exact Mass |
212.974
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| CAS # |
773-76-2
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| PubChem CID |
2722
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| Appearance |
Light brown to brown solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
354.7±37.0 °C at 760 mmHg
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| Melting Point |
178-180 °C(lit.)
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| Flash Point |
168.3±26.5 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.702
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| LogP |
3.75
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
13
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| Complexity |
191
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1=C2N=CC=CC2=C(Cl)C=C1Cl
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| InChi Key |
WDFKMLRRRCGAKS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H5Cl2NO/c10-6-4-7(11)9(13)8-5(6)2-1-3-12-8/h1-4,13H
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| Chemical Name |
5,7-dichloroquinolin-8-ol
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| Synonyms |
5,7-Dichloro-8-hydroxyquinoline; 5,7-Dichloroquinolin-8-ol; Chloroxine
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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) |
DMSO : ~33.33 mg/mL (~155.71 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (11.68 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (11.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6718 mL | 23.3590 mL | 46.7181 mL | |
| 5 mM | 0.9344 mL | 4.6718 mL | 9.3436 mL | |
| 10 mM | 0.4672 mL | 2.3359 mL | 4.6718 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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