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.
— —Written/Edited by V. Shallan【版权归集奇生物/MKBio懋康所有】