| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Haloxon targets the nervous system of parasites, specifically by inhibiting acetylcholinesterase (AChE), an enzyme essential for nerve function. Acetylcholinesterase is responsible for the breakdown of the neurotransmitter acetylcholine at synapses. By inhibiting AChE, Haloxon causes an accumulation of acetylcholine, leading to continuous stimulation of the nervous system, paralysis, and death of the parasite. This mechanism of action is common to organophosphate compounds. Haloxon's efficacy against a range of nematodes, including those of the abomasum and small intestine, is attributed to its ability to inhibit AChE in these parasites. The compound's selectivity for parasite AChE over host AChE is an important factor in its safety as a veterinary anthelmintic.
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| ln Vitro |
In vitro studies have characterized Haloxon's activity as an acetylcholinesterase inhibitor. Its activity is typically measured using enzyme assays with purified AChE from parasite or mammalian sources. The enzyme is incubated with its substrate, acetylthiocholine, in the presence of varying concentrations of Haloxon. The hydrolysis of the substrate releases thiocholine, which reacts with a chromogenic agent (e.g., DTNB) to produce a yellow color. The inhibition of enzyme activity is measured spectrophotometrically, and the IC50 is determined from the dose-response curve. In vitro assays also measure the compound's efficacy against parasitic worms in culture, assessing the ability to cause paralysis or death. These studies confirm Haloxon's mechanism of action and its potency as an anthelmintic.
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| ln Vivo |
In vivo studies have demonstrated Haloxon's efficacy as an anthelmintic in veterinary medicine. In field trials and controlled studies, Haloxon has been shown to effectively reduce the burden of nematode infections in ruminants and other domesticated animals. Its efficacy is typically measured by fecal egg count reduction (FECR) tests, where the number of parasite eggs in the feces is counted before and after treatment. Haloxon is administered orally or by injection, and its effectiveness is compared to that of other anthelmintics. The compound has been used in combination with other agents, such as Bidimazium, for the control of ascarids and hookworms. Haloxon's in vivo efficacy has made it a valuable tool in veterinary parasitology.
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| Enzyme Assay |
The in vitro enzyme assay for Haloxon measures its inhibition of acetylcholinesterase (AChE). In a typical assay, AChE is purified from a suitable source (e.g., bovine erythrocytes or parasite homogenates). The enzyme is incubated with its substrate, acetylthiocholine iodide, and the chromogenic reagent DTNB (5,5'-dithiobis-(2-nitrobenzoic acid)) in the presence of varying concentrations of Haloxon. The hydrolysis of acetylthiocholine by AChE produces thiocholine, which reacts with DTNB to form a yellow-colored product (5-thio-2-nitrobenzoic acid). The absorbance at 412 nm is measured spectrophotometrically over time. The inhibition of enzyme activity is calculated, and the IC50 is determined from the dose-response curve. This assay provides a direct measure of Haloxon's potency as an AChE inhibitor.
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| Cell Assay |
In vitro cell-based assays for Haloxon are not typically performed, as the compound's primary mechanism of action is through enzyme inhibition rather than direct effects on cells. However, the compound's effects on parasite viability can be assessed in culture. In a typical assay, parasitic worms (e.g., Haemonchus contortus or other nematodes) are maintained in culture medium. Haloxon is added at various concentrations, and the motility and survival of the worms are monitored over time. The concentration that causes paralysis or death of the worms is determined. These assays confirm the anthelmintic activity of Haloxon in a cellular context.
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| Animal Protocol |
In vivo animal experiments for Haloxon are conducted in livestock and other domesticated animals. In a typical study, animals naturally or artificially infected with gastrointestinal nematodes are randomly assigned to treatment groups. Haloxon is administered orally or by injection at a specified dose. Fecal samples are collected before treatment and at various time points after treatment to count parasite eggs (fecal egg count, FEC). The reduction in FEC in the treatment group compared to the control group is calculated as the Fecal Egg Count Reduction (FECR). The efficacy of Haloxon is determined based on the FECR. These studies are essential for evaluating the anthelmintic efficacy of Haloxon in veterinary practice.
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| ADME/Pharmacokinetics |
Haloxon has a molecular weight of 415.59 g/mol and a molecular formula of C14H14Cl3O6P. It is an organophosphate compound that is typically supplied as a solid. For research use, Haloxon is available as a neat standard. It is soluble in organic solvents. For storage, it is recommended to keep the compound at +20°C. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been studied in the context of veterinary use. Haloxon is absorbed after oral administration and is distributed to various tissues. It is metabolized in the liver and excreted in the urine and feces.
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| Toxicity/Toxicokinetics |
Haloxon is an organophosphate compound and, like other organophosphates, can be toxic to mammals, including humans. It is considered to be moderately to highly toxic. The toxicity of Haloxon is primarily due to its inhibition of acetylcholinesterase, which can lead to cholinergic crisis, characterized by symptoms such as salivation, lacrimation, urination, defecation, gastrointestinal distress, and muscle fasciculations. At high doses, it can cause respiratory depression and death. In veterinary use, the compound is administered at doses that are effective against parasites while minimizing toxicity to the host. However, care must be taken to avoid accidental exposure.
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| Additional Infomation |
Haloxon is an organophosphorus anthelmintic that has been widely used in veterinary medicine. It is effective against nematodes of the abomasum and small intestine in ruminants and is also used for the control of ascarids and hookworms in domesticated animals. Haloxon's mechanism of action involves the inhibition of acetylcholinesterase, leading to paralysis and death of the parasite. The compound is used for the research of infections of Parasarcis equorum, Oxyuris equi, and Strongylus vulgaris. Haloxon is a research compound and a veterinary drug, and it is not approved for human use. Its use in veterinary medicine has been largely replaced by newer, safer anthelmintics, but it remains a valuable research tool.
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| Molecular Formula |
C14H14CL3O6P
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| Molecular Weight |
415.59016
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| Exact Mass |
413.959
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| CAS # |
321-55-1
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| PubChem CID |
9454
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| Appearance |
White to off-white solid powder
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| Density |
1.5g/cm3
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| Boiling Point |
504.6ºC at 760 mmHg
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| Flash Point |
438.8ºC
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| Index of Refraction |
1.561
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| LogP |
4.752
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
24
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| Complexity |
529
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=P(OCCCl)(OC1=CC=C(C(O2)=C1)C(C)=C(Cl)C2=O)OCCCl
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| InChi Key |
KULDXINYXFTXMO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14Cl3O6P/c1-9-11-3-2-10(8-12(11)22-14(18)13(9)17)23-24(19,20-6-4-15)21-7-5-16/h2-3,8H,4-7H2,1H3
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| Chemical Name |
bis(2-chloroethyl) (3-chloro-4-methyl-2-oxochromen-7-yl) phosphate
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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 mg/mL (~79.41 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 | 2.4062 mL | 12.0311 mL | 24.0622 mL | |
| 5 mM | 0.4812 mL | 2.4062 mL | 4.8124 mL | |
| 10 mM | 0.2406 mL | 1.2031 mL | 2.4062 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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