産品簡介:
Diphenyleneiodonium
Chloride (DPI) 二苯基氯化碘鹽
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産品标簽
DPI 二苯基氯化碘鹽;iNOS/eNOS抑制劑;NADPH氧化酶;GPR3 agonist GPR3激動劑; CAS:4673-26-1;
産品信息
産品名稱
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産品編号
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CAS NO.
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規格
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價格(元)
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Diphenyleneiodonium Chloride (DPI) 二苯基氯化碘鹽
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MZ2701-10MG
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4673-26-1
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10mg
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988
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Diphenyleneiodonium Chloride (DPI) 二苯基氯化碘鹽
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MZ2701-50MG
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4673-26-1
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50mg
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2988
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産品描述
二苯基氯化碘鹽(Diphenyleneiodonium Chloride, DPI)是一(yī)種不可逆的iNOS和eNOS抑制劑,IC50分别是50nM和0.3µM,其抑制是有效的、不可逆的,時間和溫度依賴性的。NADPH,NADP+和2'5'-ADP能(néng)夠阻斷DPI的抑制活性。類似的,FAD或FMN能(néng)保護NOS不被DPI抑制[1]。DPI結合并抑制中性粒細胞NADPH氧化酶[2]。DPI是一(yī)種GPR3激動劑(EC50=1μM)。通(tōng)過GPR3(但不是GPR6或GPR12)活化腺苷酸環化酶,能(néng)夠誘導鈣動員(yuán)和β-arrestin受體内在化[3]。DPI抑制IL-1β誘導的NFκB活化[4]。齧齒類模型中預防早期酒精性肝損傷。
産品特性
1) CAS NO:4673-26-1
2) 化學名:1,1'-Biphenyl]-2,2'-diyliodonium chloride
3) 同義名:DPI chloride; Dibenziodolium chloride; 氯化二亞苯基碘鎓;二亞苯基碘鎓氯化物(wù);
4) 分子式:C12H8I·Cl
5)
分子量:314.55 g/mol
6)
純度:>98%
7)
外觀:白(bái)色至類白(bái)色粉末
8) 溶解性:溶于DMSO(>10 mM,可能(néng)需要加熱和超聲助溶)【“>”:表明溶于标示濃度,但飽和溶解度未知。】
9) 結構式:
保存與運輸方法
保存:-20ºC幹燥保存,3年(nián)有效。
運輸:常溫運輸。
注意事(shì)項
1)
為(wèi)了讓化合物(wù)更好的溶解,可通(tōng)過37℃加熱或(和)超聲波水(shuǐ)浴中震動片刻來處理。若實驗所需濃度過大甚至達産品溶解極限,請添加助溶劑助溶或自(zì)行調整濃度。
2) 本品僅用作科研用途,不得用作臨床診斷或治療,不得用于食品或藥品,絕對禁止用在人身上(shàng)。
3)
為(wèi)了您的安全和健康,請穿實驗服并戴一(yī)次性手套操作。
配制儲存液
質量
溶劑體積
濃度
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1mg
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5mg
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10mg
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1mM
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3.1791
mL
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15.8957
mL
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31.7914
mL
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5mM
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0.6358
mL
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3.1791
mL
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6.3583 mL
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10mM
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0.3179
mL
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0.5403
mL
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3.1791
mL
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使用方法【源自(zì)文獻,僅作參考】
文獻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
體外研究(細胞實驗):
細胞類型(Cell type):U2OS cells
藥物(wù)配制(Preparation):DPI was dissolved in DMSO to make stock solution and stored at
-20℃.
實驗方法(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.
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文獻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
體内研究(動物(wù)模型):
動物(wù)模型(Animal Model):ddy mice (6–7 wk of age)
實驗方法(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.
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參考文獻
[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【版權歸MKBio懋康所有】
上海夢澤生物科技有限公司是一(yī)家涉足于生(shēng)命科學和生(shēng)物(wù)技(jì)術(shù)領域研究的試劑、儀器(qì)和實驗室消耗品與實驗服務工(gōng)作,主要從(cóng)事(shì)細胞生(shēng)物(wù)學、植物(wù)學、分子生(shēng)物(wù)學、免疫學、生(shēng)物(wù)化學、蛋白(bái)組學。生(shēng)物(wù)制藥與診斷試劑研發生(shēng)産等領域。 本公司秉承“以人為(wèi)本,以誠為(wèi)信、合同守信”的經營理念。堅持"品質保障"的原則為(wèi)廣大客戶提供優質産品。
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