Temephos-d12
Temephos-d12 is the deuterium labeled Temephos. Temephos (Temefos) is an orally active, blood-brain barrier-permeable organophosphate insecticide and AChE inhibitor. By irreversibly inhibiting AChE to induce cholinergic overactivation, Temephos effectively blocks larval development of Aedes aegypti (yellow fever mosquito) and Aedes albopictus (Asian tiger mosquito), and is commonly used in studies related to Dengue Virus, Zika Virus and other relevant pathogens. Temephos exhibits genotoxicity and neurodevelopmental toxicity, and may also cause liver injury, reproductive system abnormalities and cholinergic poisoning symptoms in mammals. Temephos tends to accumulate in adipose tissues and aquatic organisms, and is excreted via feces after metabolism through oxidation and hydrolysis. Note that CYP-mediated metabolic detoxification may reduce the actual larvicidal efficacy of Temephos against some mosquito species. Temephos can be used in research related to dengue fever, Zika virus disease, chikungunya and dracunculiasis.
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- CAS No.: 1219795-39-7
- Formule: C16H8D12O6P2S3
- Masse moléculaire:478.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1219795-39-7
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Unlabeled CAS 3383-96-8
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Masse moléculaire 478.54
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Formule C16H8D12O6P2S3
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SMILES
[2H]C([2H])([2H])OP(OC(C=C1)=CC=C1SC(C=C2)=CC=C2OP(OC([2H])([2H])[2H])(OC([2H])([2H])[2H])=S)(OC([2H])([2H])[2H])=S
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Synonyms
Temefos-d12
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Pureté et documentation
Références
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[4]. Grisales N, et al. Temephos resistance in Aedes aegypti in Colombia compromises dengue vector control. PLoS Negl Trop Dis. 2013;7(9):e2438. Published 2013 Sep 19. [Content Brief]
[5]. Verdín-Betancourt FA, et al. Toxicokinetics of temephos after oral administration to adult male rats. Arch Toxicol. 2021;95(3):935-947. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)