Tralopyril
Based on 1 Customer Validation
Tralopyril is an orally active, blood-brain barrier-penetrating antifouling insecticide and endocrine disruptor. By interfering with the thyroid hormone system and mitochondrial oxidative phosphorylation, Tralopyril downregulates the transcription of genes such as TRHR, Nkx2.1, TRα and induces ferroptosis. Tralopyril disrupts amino acid, energy and lipid metabolism, exhibits significant skeletal and reproductive toxicity, and causes developmental damage. Tralopyril has a long half-life in vivo and wide tissue distribution, posing potential risks to aquatic organisms and human health. Tralopyril shows species specificity in in vitro liver microsomal metabolism, exerts lethal effects on target insects and laboratory animals, and is commonly used in studies of chlorfenapyr poisoning and related toxic mechanisms.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.70%
- CAS 番号: 122454-29-9
- 分子式: C12H5BrClF3N2
- 分子量:349.53
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
Tralopyril potently inhibits growth, ATP production, and effective quantum yield in Chlamydomonas reinhardtii cells[1].
Tralopyril (200 μM; 0, 5, 15, 30, 45, 60 min) exhibits low metabolic clearance in human and monkey liver microsomes, moderate clearance in mouse, rat, and dog liver microsomes, with interspecies differences in in vitro metabolic stability[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tralopyril (45 mg/kg; p.o.), the in vivo metabolite of chlorfenapyr, has a significantly longer half-life (5.39 h), higher AUC0-t, and higher Cmax than chlorfenapyr, and it distributes widely across all mouse tissues including the brain[3].
Tralopyril (27 mg/kg; p.o.; single dose) has an oral LD50 of 27 mg/kg in male rats, indicating acute lethal toxicity via this route[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 8-9 weeks old, 22-25 g, SPF-grade)[3]
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Dosage:45 mg/kg (generated in vivo via metabolic conversion of chlorfenapyr)
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Administration:p.o.
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Result:Exhibited a half-life of 5.39 h, area under the curve (AUC(0-t)) of 15912.77 μg/L*h, peak concentration (Cmax) of 4212.48 μg/L, and time to peak concentration (Tmax) of 0.42 h.
Was widely distributed across all tested tissues (heart, liver, spleen, lung, kidney, brain, skeletal muscle, stomach, intestine, plasma), including crossing the blood-brain barrier.
Was cleared more slowly than chlorfenapyr, with detectable levels in most tissues for up to 24 hours post-administration.
化学情報
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CAS 番号 122454-29-9
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性状 Solid
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分子量 349.53
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分子式 C12H5BrClF3N2
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Color White to off-white
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SMILES
C1=C(C=CC(=C1)Cl)C2=C(C#N)C(=C(C(F)(F)F)N2)Br
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 8.75 mg/mL (25.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (394 KB)
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- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chen X, et al. Tralopyril induces developmental toxicity in zebrafish embryo (Danio rerio) by disrupting the thyroid system and metabolism. Sci Total Environ. 2020;746:141860. [Content Brief]
[3]. Zhang S, et al. Toxicokinetics, in vivo metabolic profiling and tissue distribution of chlorfenapyr in mice. Arch Toxicol. 2024;98(11):3763-3775. [Content Brief]
[4]. Chung MJ, et al. A Fatal Case of Chlorfenapyr Poisoning and the Therapeutic Implications of Serum Chlorfenapyr and Tralopyril Levels. Medicina (Kaunas). 2022;58(11):1630. Published 2022 Nov 11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8610 mL | 14.3049 mL | 28.6098 mL | 71.5246 mL |
| 5 mM | 0.5722 mL | 2.8610 mL | 5.7220 mL | 14.3049 mL | |
| 10 mM | 0.2861 mL | 1.4305 mL | 2.8610 mL | 7.1525 mL | |
| 15 mM | 0.1907 mL | 0.9537 mL | 1.9073 mL | 4.7683 mL | |
| 20 mM | 0.1430 mL | 0.7152 mL | 1.4305 mL | 3.5762 mL | |
| 25 mM | 0.1144 mL | 0.5722 mL | 1.1444 mL | 2.8610 mL |