描述
Diphenyleneiodonium Chloride (DPI) 二苯基氯化碘盐
产品标签
DPI 二苯基氯化碘盐;iNOS/eNOS抑制剂;NADPH氧化酶;GPR3 agonist GPR3激动剂; CAS:4673-26-1;
产品信息
产品名称 | 产品编号 | CAS NO. | 规格 | 价格(元) |
Diphenyleneiodonium Chloride (DPI) 二苯基氯化碘盐 | MZ2701-10MG | 4673-26-1 | 10mg | 988 |
Diphenyleneiodonium Chloride (DPI) 二苯基氯化碘盐 | MZ2701-50MG | 4673-26-1 | 50mg | 2988 |
产品描述
二苯基氯化碘盐(Diphenyleneiodonium Chloride, DPI)是一种不可逆的iNOS和eNOS抑制剂,IC50分别是50nM和0.3µM,其抑制是有效的、不可逆的,时间和温度依赖性的。NADPH,NADP+和2’5′-ADP能够阻断DPI的抑制活性。类似的,FAD或FMN能保护NOS不被DPI抑制[1]。DPI结合并抑制中性粒细胞NADPH氧化酶[2]。DPI是一种GPR3激动剂(EC50=1μM)。通过GPR3(但不是GPR6或GPR12)活化腺苷酸环化酶,能够诱导钙动员和β-arrestin受体内在化[3]。DPI抑制IL-1β诱导的NFκB活化[4]。啮齿类模型中预防早期酒精性肝损伤。
产品特性
1) CAS NO:4673-26-1
2) 化学名:1,1′-Biphenyl]-2,2′-diyliodonium chloride
3) 同义名:DPI chloride; Dibenziodolium chloride; 氯化二亚苯基碘鎓;二亚苯基碘鎓氯化物;
4) 分子式:C12H8I·Cl
5) 分子量:314.55 g/mol
6) 纯度:>98%
7) 外观:白色至类白色粉末
8) 溶解性:溶于DMSO(>10 mM,可能需要加热和超声助溶)【“>”:表明溶于标示浓度,但饱和溶解度未知。】
9) 结构式:
保存与运输方法
保存:-20ºC干燥保存,3年有效。
运输:常温运输。
注意事项
1) 为了让化合物更好的溶解,可通过37℃加热或(和)超声波水浴中震动片刻来处理。若实验所需浓度过大甚至达产品溶解极限,请添加助溶剂助溶或自行调整浓度。
2) 本品仅用作科研用途,不得用作临床诊断或治疗,不得用于食品或药品,绝对禁止用在人身上。
3) 为了您的安全和健康,请穿实验服并戴一次性手套操作。
配制储存液
质量
溶剂体积 浓度 |
1mg | 5mg | 10mg |
1mM | 3.1791 mL | 15.8957 mL | 31.7914 mL |
5mM | 0.6358 mL | 3.1791 mL | 6.3583 mL |
10mM | 0.3179 mL | 0.5403 mL | 3.1791 mL |
使用方法【源自文献,仅作参考】
文献1,Ye C et al. Identification of a novel small-molecule agonist for human G protein-coupled receptor 3. J Pharmacol Exp Ther. 2014 Jun;349(3):437-43.PMID: 24633425
体外研究(细胞实验): 细胞类型(Cell type):U2OS cells 药物配制(Preparation):DPI was dissolved in DMSO to make stock solution and stored at -20℃. 实验方法(Assay):U2OS cells were seeded onto glass coverslips in 24-well plates and transfected with plasmids encoding FLAG-GPR3-GFP. Thirty-six hours later, cells were changed into Dulbecco’s modified Eagle’s medium containing 0.5% FBS at 37°C for 2 hours followed by 1-hour incubation in mediacontaining DPI (10 μM) or vehicle [0.1% dimethylsulfoxide (DMSO)].Cells were then washed three times with phosphate-buffered saline and fixed in 4% paraformaldehyde. After counterstaining of nuclei with Hoechst dye 33342, cells were examined using an FV10i confocal microscope. |
文献2,Deng CC et al.Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006. PMID: 23831840
体内研究(动物模型): 动物模型(Animal Model):ddy mice (6–7 wk of age) 实验方法(Assay):The ddy mice (6–7 wk of age) were individually placed in transparent cages for 30 min before experiments.An intraplantar injection of 10 μl DPI (2 mM, solvent: Kolliphor EL with 20% DMSO) was then injected into the right hindpaw with or without intraperitoneal administration with HC030031 (300 mg/kg at 0.5 h prior to injection of DPI; solvent: saline with 0.5% methyl cellulose).The time spent licking or biting the injected paw was recorded for 45 min after injection. |
参考文献
[1] Stuehr DJ et al. Inhibition of macrophage and endothelial cell nitric oxide synthase by diphenyleneiodonium and its analogs. FASEB J. 1991 Jan;5(1):98-103.
[2] Yea CM et al. Purification and some properties of the 45 kDa diphenylene iodonium-binding flavoprotein of neutrophil NADPH oxidase. Biochem J. 1990 Jan 1;265(1):95-100.
[3] Ye C et al. Identification of a novel small-molecule agonist for human G protein-coupled receptor 3. J Pharmacol Exp Ther. 2014 Jun;349(3):437-43.
[4] Mendes AF et al. Diphenyleneiodonium inhibits NF-kappaB activation and iNOS expression induced by IL-1beta: involvement of reactive oxygen species. Mediators Inflamm. 2001 Aug;10(4):209-15.
[5] Kono H et al. Diphenyleneiodonium sulfate, an NADPH oxidase inhibitor, prevents early alcohol-induced liver injury in the rat. Am J Physiol Gastrointest Liver Physiol. 2001 May;280(5):G1005-12.