1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDiphenyleneiodonium chlorideCat. No.: HY-100965CAS No.: 4673-26-1Synonyms: DPI分式: CHClI分量: 314.55作靶點(diǎn): TRP Channel; NADPH Oxidase作通路: Membrane Transporter/Ion Channel; Neuronal Signaling;Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C

2、3 years4C 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)Mass Solvent1 mg 5 mg 10 mg Concentration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(qǐng)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，并請(qǐng)注

3、意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Diphenyleneiodonium chloride種 NADPH 氧化酶 (NOX) 抑制劑，也 種 TRPA1 激活劑，EC50 值在 1 3 M 之間。IC50 & Target NOX 1EC50: 1 to 3 M (TRPA1) 11/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a

4、 TRPA1 activatorwith an EC50 of 1 to 3 M. Application of Diphenyleneiodonium chloride to HEK-TRPA1 cells at aconcentration ranges of 0.03 to 10 M effectively induces a Ca2+ response. However, Diphenyleneiodoniumchloride fails to evoke a Ca2+ response in control HEK cells, even at a relatively high d

5、ose of 10 M 1.When Diphenyleneiodonium chloride is included in the co-cultures, lipopolysaccharide (LPS)-induced preOLapoptosis is significantly inhibited. Treatment with Diphenyleneiodonium chloride is found to significantlyattenuate the LPS-induced O2- production by 2.0-fold, reducing it to within

6、 27% of the controls 2.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 lipopolysaccharide (LPS) injectionsignificantly attenuates the LPS-induced loss of O4 positive c

7、ells. Treatment with Diphenyleneiodoniumchloride either immediately or 24 h after LPS injection significantly ameliorates the LPS-induceddisorganization of the white matter nerve fibers. However, treatment with DPI 48 h after LPS injection doesnot appear to correct the LPS-induced white matter damag

8、e. DPI treatment either immediately or 24 h afterLPS injection significantly reduces the accumulation of both gp91phox and p67phox in the membranefraction 2.PROTOCOLCell Assay 2 Purified microglia and preOLs are co-cultured using a Transwell culture system. Co-cultured cells are dividedinto three gr

9、oups: control, lipopolysaccharide (LPS)-activated, and LPS plus Diphenyleneiodonium chloride.Microglia are cultured in Transwells over established preOL layers and exposed to either LPS (100 ng/mL),LPS+Diphenyleneiodonium chloride (10 M) or untreated. The medium supernatants and cellular proteinfrac

10、tions from the co-cultures are then collected for further analysis after 48 h incubation 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal The ddy mice (6 to 7 wk of age) are individually placed in transparent cages for 30 min before experiments.

11、Administration 1 An intraplantar injection of 10 L Diphenyleneiodonium chloride (2 mM, solvent: Kolliphor EL with 20%DMSO) is then injected into the right hindpaw with or without intraperitoneal administration with HC030031(300 mg/kg at 0.5 h prior to injection of Diphenyleneiodonium chloride; solve

12、nt: saline with 0.5% methylcellulose). The time spent licking or biting the injected paw is recorded for 45 min after injection 1.MCE has not independently confirmed the accuracy of these methods. They are for reference 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.

13、 2018 Mar 1;314(3):H580-H592. Toxicol Appl Pharmacol. 2019 Mar 1;366:83-95.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Suzuki H, et al. The NADPH oxidase inhibitor diphenyleneiodonium activates the human TRPA1 nociceptor. Am J Physiol Cell Physiol.2014 Aug 15;307(4):C384-94.2. He YF, et al. Diphenyleneiodonium protects preoligodendrocytes against endotoxin-activated microglial NADPH oxidase-generatedperoxynitrite in a neonatal rat model of periventricular leukomalacia. Brain Res. 2013 Jan 25;1492: