| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Amitraz targets alpha-2 adrenergic receptors in the central nervous system of parasites. It acts as an agonist at these receptors, leading to excessive stimulation and paralysis of the parasite. Amitraz also inhibits monoamine oxidase (MAO), an enzyme that breaks down monoamine neurotransmitters. The combination of alpha-2 adrenergic agonism and MAO inhibition results in the death of the parasite. Amitraz has a selective toxicity for invertebrates over vertebrates.
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|---|---|
| ln Vitro |
In vitro, Amitraz has been shown to bind to alpha-2 adrenergic receptors and to inhibit monoamine oxidase activity. It causes paralysis and death of ticks and mites in vitro. The compound's acaricidal activity has been demonstrated against various species of ticks, including Rhipicephalus and Ixodes species. Amitraz also has insecticidal activity against lice and other ectoparasites. Its activity is concentration-dependent.
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| ln Vivo |
In vivo, Amitraz is used in veterinary medicine for the control of ectoparasitic infestations. It is effective against ticks, mites, and lice in cattle, sheep, dogs, and other animals. Amitraz is applied topically as a dip, spray, or pour-on formulation. It has also been used in agriculture to control pests on crops. Amitraz has a rapid onset of action and provides prolonged protection against re-infestation.
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| Enzyme Assay |
In vitro acaricidal assays for Amitraz typically involve exposing ticks or mites to various concentrations of the compound and assessing mortality over time. The compound is dissolved in an appropriate solvent and applied to the parasites. The LC50 (concentration required to kill 50% of the parasites) is determined from dose-response curves. The effect of amitraz on parasite behavior and physiology can also be studied.
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| Cell Assay |
In vitro cell-based studies with Amitraz are limited, as the compound is primarily used as a pesticide rather than a drug. However, its effects on mammalian cells can be studied to assess its toxicity. Cells are treated with Amitraz at various concentrations, and cell viability is assessed using MTT or similar assays. The effect of the compound on alpha-2 adrenergic receptor signaling can be studied in cells expressing these receptors.
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| Animal Protocol |
In vivo animal studies with Amitraz are typically conducted in veterinary settings to evaluate its efficacy against ectoparasites. Animals are treated with Amitraz by topical application, and the reduction in parasite burden is assessed. The compound's safety and tolerability in animals are also evaluated. Pharmacokinetic studies are performed to measure amitraz levels in blood and tissues.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Amitraz have been studied in animals. Following topical application, it is absorbed through the skin and distributed to various tissues. Amitraz is metabolized in the liver to various metabolites, including 2,4-dimethylaniline (DMA) and N-(2,4-dimethylphenyl)-N-methylformamidine (DMPF). The compound and its metabolites are excreted in the urine. The half-life of amitraz in animals is relatively short.
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| Toxicity/Toxicokinetics |
The toxicity of Amitraz has been evaluated in animals. The compound has a relatively low toxicity in mammals when used at recommended doses. However, Amitraz can cause adverse effects, including sedation, bradycardia, and hyperglycemia, due to its alpha-2 adrenergic agonist activity. Overdose can lead to more severe effects, including respiratory depression and coma. Appropriate safety precautions should be taken when handling the compound.
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| Additional Infomation |
According to the U.S. Environmental Protection Agency (EPA), amectorazole may cause developmental toxicity. Amectorazole is a tertiary amine compound with the structure 1,3,5-triazapent-1,4-diene, substituted with a methyl group at the 3-position and substituted with 2,4-dimethylphenyl groups at the 1- and 5-positions. It is used as an acaricide, exogenous substance, environmental pollutant, and insecticide. It is a tertiary amine compound belonging to the formamidinaceae class of compounds. See also: Amectorazole (note moved to).
Amitraz is a widely used acaricide and insecticide in veterinary medicine and agriculture. It is effective against a broad range of ectoparasites, including ticks, mites, and lice. Amitraz is available in various formulations for topical application. The compound is not approved for use in humans. Amitraz is an important tool for the control of ectoparasites in livestock and pets and is also used in crop protection. |
| Molecular Formula |
C19H23N3
|
|---|---|
| Molecular Weight |
293.41
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| Exact Mass |
293.189
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| CAS # |
33089-61-1
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| Related CAS # |
Amitraz-d3
|
| PubChem CID |
36324
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| Appearance |
White to light yellow solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
450.7±55.0 °C at 760 mmHg
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| Melting Point |
86-87°C
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| Flash Point |
226.4±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.546
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| LogP |
5.64
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
22
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| Complexity |
354
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
QXAITBQSYVNQDR-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H23N3/c1-14-6-8-18(16(3)10-14)20-12-22(5)13-21-19-9-7-15(2)11-17(19)4/h6-13H,1-5H3
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| Chemical Name |
N'-(2,4-dimethylphenyl)-N-[(2,4-dimethylphenyl)iminomethyl]-N-methylmethanimidamide
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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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~340.82 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.52 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 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 (8.52 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4082 mL | 17.0410 mL | 34.0820 mL | |
| 5 mM | 0.6816 mL | 3.4082 mL | 6.8164 mL | |
| 10 mM | 0.3408 mL | 1.7041 mL | 3.4082 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03959891 | Active, not recruiting | Drug: Ipatasertib Drug: Fulvestrant Drug: Aromatase Inhibitor Drug: Palbociclib |
Breast Cancer | Massachusetts General Hospital | 2019-05-30 | Phase 1 |
| NCT01980277 | Terminated | Drug: LY2780301 + paclitaxel | Breast Cancer | Institut Paoli-Calmettes | 2014-01 | Phase 1 Phase 2 |
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