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双香豆素 /Dicoumarol {[allProObj[0].p_purity_real_show]}

货号:A205533 同义名: 双羟香豆素 / Dicumarol;NSC 17860

Dicoumarolis a widely used potent competitive NQO1 inhibitor.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Dicoumarol 化学结构 CAS号:66-76-2
Dicoumarol 化学结构
CAS号:66-76-2
Dicoumarol 3D分子结构
CAS号:66-76-2
Dicoumarol 化学结构 CAS号:66-76-2
Dicoumarol 3D分子结构 CAS号:66-76-2
规格 价格 会员价 库存 数量
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Dicoumarol 纯度/质量文件 产品仅供科研

货号:A205533 标准纯度: {[allProObj[0].p_purity_real_show]}
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Dicoumarol 生物活性

描述 Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively[3]. DIC (Dicoumarol) potently inhibited the kinase activity of PDK1(Pyruvate dehydrogenase kinase 1), shifted the glucose metabolism from aerobic glycolysis to oxidative phosphorylation, generated a higher level of reactive oxygen species (ROS), attenuated the mitochondrial membrane potential (MMP), induced apoptosis, and reduced cell viability in vitro[4]. Exposure of erythrocytes for 48 hours to dicoumarol (=10 μM) significantly increased [Ca(2+)](i), enhanced cation channel activity, decreased forward scatter, triggered annexin-V-binding and elicited hemolysis. Dicoumarol stimulates suicidal death of erythrocytes by stimulating Ca(2+) entry and subsequent triggering of Ca(2+) dependent cell membrane scrambling[5]. Moreover, dicoumarol synergized with emodin to sensitize HeLa cells to As2O3(arsenic trioxide)-induced apoptosis through raising the ROS (reactive oxygen species) level[6].

Dicoumarol 参考文献

[1]Bian J, Li X, et al. Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation. Eur J Med Chem. 2017 Feb 15;127:828-839.

[2]Zhang W, Su J, et al. Dicumarol inhibits PDK1 and targets multiple malignant behaviors of ovarian cancer cells. PLoS One. 2017 Jun 15;12(6):e0179672.

[3]Bian J, Li X, Xu L, Wang N, Qian X, You Q, Zhang X. Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation. Eur J Med Chem. 2017 Feb 15;127:828-839

[4]Zhang W, Su J, Xu H, Yu S, Liu Y, Zhang Y, Sun L, Yue Y, Zhou X. Dicumarol inhibits PDK1 and targets multiple malignant behaviors of ovarian cancer cells. PLoS One. 2017 Jun 15;12(6):e0179672

[5]Qadri SM, Kucherenko Y, Zelenak C, Jilani K, Lang E, Lang F. Dicoumarol activates Ca2+-permeable cation channels triggering erythrocyte cell membrane scrambling. Cell Physiol Biochem. 2011;28(5):857-64

[6]Jing YW, Yi J, Chen YY, Hu QS, Shi GY, Li H, Tang XM. Dicoumarol alters cellular redox state and inhibits nuclear factor kappa B to enhance arsenic trioxide-induced apoptosis. Acta Biochim Biophys Sin (Shanghai). 2004 Mar;36(3):235-42

Dicoumarol 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.87mL

2.97mL

1.49mL

29.74mL

5.95mL

2.97mL

Dicoumarol 技术信息

CAS号66-76-2
分子式C19H12O6
分子量 336.295
别名 双羟香豆素 ;Dicumarol;NSC 17860;Antitrombosin;Melitoxin;Dicoumarin;Bishydroxycoumarin;NSC 221570;NSC 41834
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 3 mg/mL(8.92 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(74.34 mM),配合低频超声,并调节pH至11

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

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