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Dicoumarol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dicoumarol图片
CAS NO:66-76-2
包装与价格:
包装价格(元)
500mg电议
1 g电议
5 g电议

产品名称
双香豆素
Dicumarol
产品介绍
Dicoumarol 是 NAD(P)H: 醌氧化还原酶 1 (NQO1) 和PDK1的抑制剂,IC50值分别为 0.37 和 19.42 μM。
生物活性

Dicoumarol is an inhibitor of bothNAD(P)H:quinone oxidoreductase 1(NQO1) andPDK1withIC50s of 0.37 and 19.42 μM, respectively.

IC50& Target

IC50: 0.37 μM (NQO1)[1], 19.42 μM (PDK1)[2]

体外研究
(In Vitro)

Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37±0.15 and 19.42±0.032 μM, respectively. The PDK1 activity is inhibited by Dicoumarol in a dose-dependent manner. The enzymatic activity of PDK1 is reduced by approximately 94% when treated with 200 μM Dicoumarol. Dicoumarol decreases the p-PDHA1 level by 26% (100 μM Dicoumarol) and by 72% (200 μM Dicoumarol), with no statistical difference in the total PDHA1 level. Both 100 μM and 200 μM Dicoumarol markedly induce apoptosis of SKOV3 cells. Similarly, flow cytometric analysis of annexin V+PI+cells reveals that 100 μM and 200 μM Dicoumarol treatments generate approximately 20.87% and 24.94% apoptotic cells, respectively, significantly higher than vehicle treatment[2]. It is also observed that treatment of MCF-7-TAMR cells with Dicoumarol, a known NQO1 inhibitor, reverses their tamoxifen-resistance phenotype[3].

体内研究
(In Vivo)

Dichloroacetate (DCA) at 100 mg/kg, Dicoumarol at 30 mg/kg, and Dicoumarol at 50 mg/kg all significantly reduce tumor volume and decrease tumor weight, when compare to tumors from control or vehicle groups. Total caspase-3 and total anti-poly (ADP-ribose) polymerase (PARP) are significantly decreased in Dicoumarol-treated SKOV3 xenografts, when compare to tumors from the control or vehicle group[2].

分子量

336.29

性状

Solid

Formula

C19H12O6

CAS 号

66-76-2

结构分类
  • Phenylpropanoids
  • Coumarins
来源
  • Plants
  • Leguminosae
  • Melilotus officinalis(L.) Pall.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

H2O : 25 mg/mL(74.34 mM;ultrasonic and adjust pH to 11 with NaOH)

DMSO : 3.67 mg/mL(10.91 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.9736 mL14.8681 mL29.7362 mL
5 mM0.5947 mL2.9736 mL5.9472 mL
10 mM0.2974 mL1.4868 mL2.9736 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。