產品簡介:
Diphenyleneiodonium
Chloride (DPI) 二苯基氯化碘鹽
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產品標簽
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;
產品信息
產品名稱
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產品編號
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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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產品描述
二苯基氯化碘鹽(Diphenyleneiodonium Chloride, DPI)是一種不可逆的iNOS和eNOS抑制劑,IC50分別是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能夠阻斷DPI的抑制活性。類似的,FAD或FMN能保護NOS不被DPI抑制[1]。DPI結合并抑制中性粒細胞NADPH氧化酶[2]。DPI是一種GPR3激動劑(EC50=1μM)。通過GPR3(但不是GPR6或GPR12)活化腺苷酸環化酶,能夠誘導鈣動員和β-arrestin受體內在化[3]。DPI抑制IL-1β誘導的NFκB活化[4]。嚙齒類模型中預防早期酒精性肝損傷。
產品特性
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;
4) 分子式:C12H8I·Cl
5)
分子量:314.55 g/mol
6)
純度:>98%
7)
外觀:白色至類白色粉末
8) 溶解性:溶于DMSO(>10 mM,可能需要加熱和超聲助溶)【“>”:表明溶于標示濃度,但飽和溶解度未知?!?/span>
9) 結構式:
保存與運輸方法
保存:-20oC干燥保存,3年有效。
運輸:常溫運輸。
注意事項
1)
為了讓化合物更好的溶解,可通過37℃加熱或(和)超聲波水浴中震動片刻來處理。若實驗所需濃度過大甚至達產品溶解極限,請添加助溶劑助溶或自行調整濃度。
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。
3)
為了您的安全和健康,請穿實驗服并戴一次性手套操作。
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
體內研究(動物模型):
動物模型(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】
上海懋康生物科技有限公司是一家涉足于生命科學和生物技術領域研究的試劑、儀器和實驗室消耗品與實驗服務工作,主要從事細胞生物學、植物學、分子生物學、免疫學、生物化學、蛋白組學。生物制藥與診斷試劑研發生產等領域。 本公司秉承“以人為本,以誠為信、合同守信”的經營理念。堅持"品質保障"的原則為廣大客戶提供優質產品。
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