| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Halazone targets carbonic anhydrase II (CA-II) with a Kd of 1.45 µM. It also modulates voltage-gated sodium channels in electrophysiological models. As a chlorine-releasing agent, its primary mechanism of action involves hydrolysis of its nitrogen-chlorine bonds upon dissolution in water, liberating hypochlorous acid (HOCl) which acts as a potent disinfectant. This makes it effective against a broad spectrum of microorganisms, including E. coli, typhoid bacilli, and cholera vibrio.
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| ln Vitro |
Halazone is chemically similar to Chloramine-T; however, instead of one chlorine atom connecting the nitrogen atom, two are linked, and—perhaps more importantly—a carboxyl group takes the place of a methyl group. The study examines the impact of Halazone on sodium current in frog voltage-clamped single nerve fibers. Inactivation is significantly inhibited by the oxidant halazone[1].
In vitro, Halazone exhibits potent antibacterial activity as a water disinfectant. It inhibits carbonic anhydrase II with a Kd of 1.45 µM. At concentrations of 1:200,000 to 1:500,000, it can kill E. coli, typhoid bacilli, paratyphoid bacilli, cholera vibrio, and Shigella within 0.5 to 1 hour. It shows 2-fold faster bacterial kill compared to bleaching powder at equivalent free chlorine dose and has proven efficacy against Giardia cysts. |
| ln Vivo |
In vivo data for Halazone is derived from its historical use as a water disinfectant in military and emergency scenarios. It has been used for drinking water disinfection, demonstrating efficacy against waterborne pathogens. However, specific published in vivo efficacy studies in animal models are not detailed in the current literature. Halazone is primarily used as a research tool for studying carbonic anhydrase inhibition and water disinfection, with its use as a therapeutic agent being historical.
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| Enzyme Assay |
The in vitro carbonic anhydrase II inhibition assay for Halazone uses recombinant human carbonic anhydrase II enzyme and a suitable substrate such as 4-nitrophenyl acetate. Enzyme activity is measured spectrophotometrically, and Kd values are calculated from binding studies using surface plasmon resonance or isothermal titration calorimetry. Antibacterial activity is assessed using standard broth microdilution methods to determine minimum inhibitory concentrations (MICs) against various bacterial strains.
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| Cell Assay |
Cellular assays for Halazone are conducted in bacterial cultures and mammalian cell models. For antibacterial assays, bacteria such as E. coli are grown in appropriate media and treated with varying concentrations of Halazone. Bacterial growth inhibition is measured by optical density or colony counting. For carbonic anhydrase inhibition studies, mammalian cells expressing CA-II are treated with Halazone, and enzyme activity is measured in cell lysates. Sodium channel modulation is assessed using electrophysiological patch-clamp techniques.
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| Animal Protocol |
In vivo studies for Halazone are historical and primarily relate to its use as a water disinfectant rather than as a therapeutic agent in animal models. It was used for drinking water disinfection in military and emergency scenarios, with efficacy assessed by measuring bacterial contamination in treated water. As a research compound, Halazone would typically be administered orally in water for disinfection studies. However, specific published in vivo protocols are not detailed in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Halazone is not extensively reported in publicly available sources. The compound has a molecular weight of 270.09 g/mol and a molecular formula of C7H5Cl2NO4S. It is a fine white powder with an odor of chlorine and is insoluble in water. Stability: stable but may be light sensitive; incompatible with strong oxidizing agents. As a chlorine-releasing agent, it hydrolyzes in water to liberate HOCl. Detailed PK parameters such as half-life are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for Halazone is available from toxicological studies. The compound is an oxidizer and may be combustible. A National Toxicology Program executive summary of safety and toxicity information exists. As with all research compounds, Halazone is intended for research use only and not for human therapeutic applications. Appropriate safety precautions should be taken when handling this compound due to its chlorine-releasing properties.
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| References |
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| Additional Infomation |
Halazone is a fine white powder with a chlorine odor. (NTP, 1992)
Halazone (4-(dichlorosulfamoyl)benzoic acid) is an organic chloramine compound within the chlorine-releasing agent family, historically used as a portable water disinfectant. It is an atypical antibacterial sulfonamide analogue and an inhibitor of carbonic anhydrase II (Kd=1.45 µM). Halazone protects sodium channels from inactivation. Its disinfectant activity arises from hydrolysis of nitrogen-chlorine bonds upon dissolution, liberating hypochlorous acid (HOCl). It has a molecular formula of C7H5Cl2NO4S and a molecular weight of 270.09 g/mol. |
| Molecular Formula |
C7H5CL2NO4S
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|---|---|
| Molecular Weight |
270.09
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| Exact Mass |
268.932
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| CAS # |
80-13-7
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| PubChem CID |
3552
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| Appearance |
White to off-white solid powder
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| Density |
1.717 g/cm3
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| Boiling Point |
437ºC at 760 mmHg
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| Melting Point |
213ºC
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| Flash Point |
218.1ºC
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| LogP |
2.763
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
329
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XPDVQPODLRGWPL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H5Cl2NO4S/c8-10(9)15(13,14)6-3-1-5(2-4-6)7(11)12/h1-4H,(H,11,12)
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| Chemical Name |
4-(dichlorosulfamoyl)benzoic acid
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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: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). 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) |
DMSO : 100 mg/mL (370.25 mM)
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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 | 3.7025 mL | 18.5123 mL | 37.0247 mL | |
| 5 mM | 0.7405 mL | 3.7025 mL | 7.4049 mL | |
| 10 mM | 0.3702 mL | 1.8512 mL | 3.7025 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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