Fluensulfone-MCW-2-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFluensulfoneCat. No.: HY-107771CAS No.: 318290-98-1Synonyms: MCW-2分式: CHClFNOS分量: 291.7作靶点: Parasite作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 0.73 mg/mL (2.50 mM; Ne

2、ed ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.4282 mL 17.1409 mL 34.2818 mL5 mM - - -10 mM - - -请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Fluensulfone化学防治植物寄线的新型杀线剂。体外研究Lower concentrations of Fluensulfone delay development: 100 M Fluensulfone causes a s

3、light delay as at66 h fewer worms have reached the adult stage whilst at 300 M no worms reach the adult stage at 66 h andsome fail to reach L4. Adult hermaphrodites lay fewer eggs in the presence of 1 mM Fluensulfone.Fluensulfone is also found to reduce the viability of eggs. After 3 h incubation wi

4、th 100 M to 1 mM1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEFluensulfone the thrashing rate is significantly inhibited, with maximal inhibition occurring with 1 mM. After 1h both 300 M and 1 mM Fluensulfone cause a significant and reversible inhibition of pharyngeal pumpingrelative to the vehic

5、le control. Fluensulfone (500 M) inhibits the frequency of body bends in one day oldadult hermaphrodites off food after 2 h exposure 1.体内研究 In an in vivo investigation, female mice are treated with Fluensulfone (or isoniazid as a positive control) for 3and 7 days. Quantification of the cell prolifer

6、ation by manual counting of BrdU-positive and BrdU-negativecells in the bronchiolar epithelium reveals an approximately fourfold increase of cell proliferation upontreatment with Fluensulfone and the positive control isoniazid compare with control. Increased cellproliferation is observed at 3 days b

7、ut have reverted to the control level at day 7 2.PROTOCOLCell Assay 1 For these assays worms of different developmental stages are incubated in liquid with and withoutFluensulfone for up to 24 h, and paralysis is scored. 400 L of M9 phosphate buffer with either Fluensulfone(100 M, 200 M or 1 mM) or

8、vehicle (0.5% acetone) is put into each well of a 24 well plate (5 replicates foreach Fluensulfone concentration). 5 L suspension of age synchronised C. elegans (L1, L2/3, L4 or one dayold adult) is added to each well. Each well contains approximately 50 to100 worms. The number of wormsnot moving at

9、 1, 2, 3, 4, 5, 6 and 24 h is determined. The experiment is conducted on two separateoccasions with five replicates 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Groups of 10 female specific pathogen-free CD-1 mice each are treated with untre

10、ated diet, diet containingAdministration 2 1200 mg/kg Fluensulfone (high dose in carcinogenicity study), or 1305 mg/kg of isoniazid as a positivecontrol substance for 3 or 7 days, respectively. Two and 14 h before sacrifice, the animals are injected ip with100 L of a 10 mg/mL aqueous bromodeoxyuridi

11、ne (BrdU)-solution. Sacrifice by exsanguination under deepirreversible pentobarbital narcosis is performed early in the morning to assure that the animals are exposedto the test item until shortly before sacrifice 2.MCE has not independently confirmed the accuracy of these methods. They are for refe

12、rence only.REFERENCES1. Kearn J, et al. Fluensulfone is a nematicide with a mode of action distinct from anticholinesterases and macrocyclic lactones. PesticBiochem Physiol. 2014 Feb;109:44-57.2. Strupp C, et al. Relationship of metabolism and cell proliferation to the mode of action of fluensulfone-induced mouse lung tumors:analysis of their human relevance using the IPCS framework. Toxicol Sci. 2012 Jul;128(1):284-94.McePdfHeightCaut