Triflumuron
(Synonyms: 杀虫脲) 目录号 : GC48203
Triflumuron是一种几丁质合成抑制剂类的合成杀虫剂,其IC50值为1.48 ± 1.44μM,在对抗Culex quinquefasciatus和Aedes albopictus时的EI50值分别为5.28和1.59μg/L。
Cas No.:64628-44-0
Sample solution is provided at 25 µL, 10mM.
Triflumuron is a synthetic insecticide from the active ingredient group of chitin biosynthesis inhibitors with IC50 value of 1.48 ± 1.44μM, and with EI50 values of 5.28 and 1.59μg/L against Culex quinquefasciatus and Aedes albopictus, respectively. Triflumuron interferes with chitin synthesis and the moulting cycle, disrupting chitin deposition in the insect cuticle after ingestion[1][2][3].
In vitro, Triflumuron(1μM to 1mM) was tested for its ability to inhibit hyaluronan (HA) secretion in NIH3T3 fibroblast cells. The results showed that Triflumuron effectively reduced HA deposition in the cell culture media, with a half-maximal inhibitory concentration (IC50) of 1.48 ± 1.44μM[1]. Triflumuron (50‐300μM) treated human renal embryonic cells (HEK 293) and hepatocytes (Hep G2) reduced significantly the cell viability and increased the reactive oxygen species generation, malondialdehyde levels, and mitochondrial membrane potential in both cell lines. Triflumuron was also demonstrated as an inductor of DNA damages quantified by the comet assay[4].
In vivo, single intraperitoneal injection of Triflumuron (250, 350, 500mg/kg) in Balb/C mice induced oxidatie stress and elevated protein carbonyl levels in both liver and kidney extracts. The results also showed a significant increase in superoxide dismutase (SOD), glutathione peroxidase (GPX), glutathione S-transferase (GST) activity in liver and kidney after Triflumuron administration[5]. Triflumuron (250, 350, 500mg/kg) was administered intraperitoneally to Balb/C male mice for 24h. The results indicated that Triflumuron has genotoxic effects on mice bone marrow cells, causing DNA damage, micronuclei formation, and chromosome aberrations in a dose-dependent manner[6].
References:
[1] Tsitrina A A, Krasylov I G, Maltsev D I, et al. Inhibition of hyaluronan secretion by novel coumarin compounds and chitin synthesis inhibitors. Glycobiology. 2021 Sep 9;31(8):959-974.
[2] Belinato T A, Martins A J, Lima J B P, Valle D. Effect of triflumuron, a chitin synthesis inhibitor, on Aedes aegypti, Aedes albopictus and Culex quinquefasciatus under laboratory conditions. Parasit Vectors. 2013 Apr 4:6:83.
[3] Batra C P, Mittal P K, Adak T, Ansari M A. Efficacy of IGR compound Starycide 480 SC (Triflumuron) against mosquito larvae in clear and polluted water. J Vector Borne Dis.2005 Sep;42(3):109-16.
[4] Timoumi R, Amara I, Salem I B, Abid-Essefi S. Triflumuron induces cytotoxic effects on hepatic and renal human cell lines. J Biochem Mol Toxicol. 2020 Aug;34(8):e22504.
[5] Timoumi R, Amara I, Neffati F, et al. Acute triflumuron exposure induces oxidative stress responses in liver and kidney of Balb/C mice. Environ Sci Pollut Res Int. 2019 Feb;26(4):3723-3730.
[6] Timoumi R, Amara I, Ayed Y. et al. Triflumuron induces genotoxicity in both mice bone marrow cells and human Colon cancer cell line. Toxicol Mech Methods. 2020 Jul;30(6):438-449.
Triflumuron是一种几丁质合成抑制剂类的合成杀虫剂,其IC50值为1.48 ± 1.44μM,在对抗Culex quinquefasciatus和Aedes albopictus时的EI50值分别为5.28和1.59μg/L。Triflumuron通过干扰昆虫蜕皮过程中的几丁质沉积来发挥作用[1][2][3]。
体外实验中,Triflumuron(1μM-1mM)被用于测试其抑制NIH3T3成纤维细胞分泌透明质酸(HA)的能力,结果显示其IC50值为1.48 ± 1.44μM[1]。此外经Triflumuron(50-300μM)处理的人类肾胚胎细胞(HEK 293)和肝细胞(Hep G2)的细胞活性显著降低,同时活性氧(ROS)生成、丙二醛(MDA)水平以及线粒体膜电位均有所增加,且通过彗星实验发现其可诱导DNA损伤[4]。
体内实验中,Balb/C小鼠单次腹腔注射Triflumuron(250、350、500mg/kg)后,肝脏和肾脏提取物中的氧化应激水平和蛋白质羰基水平升高,且在Triflumuron给药后,肝脏和肾脏中的超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GPX)和谷胱甘肽S转移酶(GST)活性显著增加[5]。此外Balb/C雄性小鼠腹腔注射Triflumuron(250、350、500mg/kg)24小时后,结果表明Triflumuron对小鼠骨髓细胞具有遗传毒性,以剂量依赖性方式导致DNA损伤、微核形成和染色体畸变[6]。
Cell experiment [1]: | |
Cell lines | Hep G2 and HEK 293 cells |
Preparation Method | We used 96‐well plates to seed and incubate (2.5 × 105 cells) for 24 hours with different concentrations of Triflumuron (10-500μM) before cells were used to perform MTT assay. Triflumuron concentration range (50‐300μM) was used to treat Hep G2 and HEK 293 cells before ROS generation, antioxidant enzymes acitvities, total score of DNA damage and protein expression level were also evaluated. |
Reaction Conditions | 10 to 500µM or 50 to 300µM; 24h |
Applications | Treatment of cells with increasing concentrations of Triflumuron decreased significantly the cell viability. Triflumuron is an oxidizing agent in both renal and hepatic cells by increasing ROS production, which alters the normal functioning of antioxidant enzymes such as CAT and SOD, which consequentlydamage cells by oxidizing lipids, disrupting DNA and proteins. |
Animal experiment [2]: | |
Animal models | Male Balb/C mice |
Preparation Method | After acclimation, mice were randomly divided into four groups of six each as follows: Group 1: mice given the vehicle, ethanol/water (1:1, v:v) Groups 2, 3, and 4: mice given Triflumuron at 250, 350, and 500mg/kg bw corresponding respectively to 5, 7, and 10% of the LD50. A single administration by intra-peritoneal injection of 100μl of solutions was performed. The sacrifice was done 24h after injections by cervical dislocation. |
Dosage form | 250, 350, and 500mg/kg; i.p.; a single administration |
Applications | In treated mice, the levels of malondialdehyde (MDA), an ultimate fragment of the degradation of cell membrane polyunsaturated fatty acids, significantly increased in the liver, while only the highest dose induced lipid peroxidation in kidney tissues. Triflumuron treatment also caused protein damage via free radicals. As an adaptive response, antioxidant enzyme activities notably rose in both organs. |
References: |
Cas No. | 64628-44-0 | SDF | |
别名 | 杀虫脲 | ||
Canonical SMILES | ClC1=CC=CC=C1C(NC(NC2=CC=C(OC(F)(F)F)C=C2)=O)=O | ||
分子式 | C15H10ClF3N2O3 | 分子量 | 358.7 |
溶解度 | DMF: 30 mg/ml,DMSO: 10 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 2.7878 mL | 13.9392 mL | 27.8784 mL |
5 mM | 0.5576 mL | 2.7878 mL | 5.5757 mL |
10 mM | 0.2788 mL | 1.3939 mL | 2.7878 mL |
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