二苯基氯化碘鹽作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetDiphenyleneiodonium chlorideCat. No.: HY-100965CAS No.: 4673-26-1分式: CHClI分量: 314.55作靶點(diǎn): TRP Channel; NADPH Oxidase; Reactive Oxygen Species作通路: Membrane Transporter/Ion Channel; Neuronal Signaling; MetabolicEnzyme/Protease; Immunology/Inflammation; NF-B儲(chǔ)存式: Powder -20C 3 years4C 2

2、 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6 mg/mL (19.07 mM; Need ultrasonic and warming)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.1791 mL 15.8957 mL 31.7915 mL5 mM 0.6358 mL 3.1791 mL 6.3583 mL10 mM 0.3179 mL 1.5896 mL 3.1791 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請分裝保存，避免反復(fù)凍

3、融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)內(nèi)使。BIOLOGICAL ACTIVITY物活性 Diphenyleneiodonium chloride 種 NADPH 氧化酶 (NOX) 抑制劑，也 之間。Diphenyleneiodonium chloride 選擇性抑制胞內(nèi)活性氧。種 TRPA1 激活劑，EC50 值在 1 3 MIC & Target NOX1EC50: 1 to 3 M (TRPA1)1體外研究Diphenyleneiodonium chlorid

4、e is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with anEC50 of 1 to 3 M. Application of Diphenyleneiodonium chloride to HEK-TRPA1 cells at a concentration ranges of 0.03to 10 M effectively induces a Ca2+ response. However, Diphenyleneiodonium chloride fails to evoke a Ca

5、2+ responsein control HEK cells, even at a relatively high dose of 10 M1. When Diphenyleneiodonium chloride is included in theco-cultures, lipopolysaccharide (LPS)-induced preOL apoptosis is significantly inhibited. Treatment withPage 1 of 2 www.MedChemEDiphenyleneiodonium chloride is found to signi

6、ficantly attenuate the LPS-induced O2- production by 2.0-fold,reducing it to within 27% of the controls2.體內(nèi)研究 Intraplantar injection of 2 mM Diphenyleneiodonium chloride to the hindpaw causes licking or biting behavior1.Diphenyleneiodonium chloride treatment immediately or 24 h after lipopolysacchar

7、ide (LPS) injection significantlyattenuates the LPS-induced loss of O4 positive cells. Treatment with Diphenyleneiodonium chloride eitherimmediately or 24 h after LPS injection significantly ameliorates the LPS-induced disorganization of the white matternerve fibers. However, treatment with DPI 48 h

8、 after LPS injection does not appear to correct the LPS-induced whitematter damage. DPI treatment either immediately or 24 h after LPS injection significantly reduces the accumulation ofboth gp91phox and p67phox in the membrane fraction2.PROTOCOLCell Assay 2 Purified microglia and preOLs are co-cult

9、ured using a Transwell culture system. Co-cultured cells are divided intothree groups: control, lipopolysaccharide (LPS)-activated, and LPS plus Diphenyleneiodonium chloride. Microglia arecultured in Transwells over established preOL layers and exposed to either LPS (100 ng/mL), LPS+Diphenyleneiodon

10、ium chloride (10 M) or untreated. The medium supernatants and cellular protein fractions fromthe co-cultures are then collected for further analysis after 48 h incubation2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal The ddy mice (6 to 7 wk of

11、 age) are individually placed in transparent cages for 30 min before experiments. AnAdministration 1 intraplantar injection of 10 L Diphenyleneiodonium chloride (2 mM, solvent: Kolliphor EL with 20% DMSO) is theninjected into the right hindpaw with or without intraperitoneal administration with HC03

12、0031 (300 mg/kg at 0.5 hprior to injection of Diphenyleneiodonium chloride; solvent: saline with 0.5% methyl cellulose). The time spent lickingor biting the injected paw is recorded for 45 min after injection1.MCE has not independently confirmed the accuracy of these methods. They are for reference

13、only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Mol Plant Pathol. 2019 Jun 27. Am J Physiol Heart Circ Physiol. 2018 Mar 1;314(3):H580-H592. Biomed Pharmacother. 2019 Nov 7;121:109615. Toxicol Appl Pharmacol. 2019 Mar 1;366:83-95. Exp Cell Res. 2020 May 28;112101See more customer validations on HYPERLINK www.MedChemE www.MedChemE

14、REFERENCES1. Suzuki H, et al. The NADPH oxidase inhibitor diphenyleneiodonium activates the human TRPA1 nociceptor. Am J Physiol Cell Physiol. 2014 Aug15;307(4):C384-94.2. He YF, et al. Diphenyleneiodonium protects preoligodendrocytes against endotoxin-activated microglial NADPH oxidase-generated peroxynitrite in aneonatal rat model of periventricular leukomalacia. Brain Res. 2013 Jan 25;1492:108-21.McePdfHeightPage 2 of 3 www.M