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(E)-Flavokawain A

产品编号 T5715 CAS 37951-13-6

别名: (E)-1-(2-羟基-4,6-二甲氧基苯基)-3-(4-甲氧基苯基)-2-丙烯-1-酮, FLAVOKAVAIN A(P), 卡瓦胡椒素A

(E)-Flavokawain A 是一种来自卡瓦提取物的新型查尔酮，通过参与 Bax 蛋白依赖性和线粒体依赖性凋亡途径诱导膀胱癌细胞凋亡，并抑制小鼠肿瘤生长，具有抗癌作用。

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(E)-Flavokawain A, CAS 37951-13-6

规格	价格/CNY	货期
1 mg	￥ 153	现货
5 mg	￥ 328	现货
10 mg	￥ 613	现货
25 mg	￥ 1,090	现货
50 mg	￥ 1,630	现货
100 mg	￥ 2,450	现货
1 mL * 10 mM (in DMSO)	￥ 443	现货

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其他形式的 (E)-Flavokawain A:

Flavokawain A
现货

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纯度: 99.7%

纯度: 98%

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天然产物信息

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

植物来源	天然产物 > 胡椒科 > 胡椒属
结构类型	天然产物 > 其他

产品描述	(E)-Flavokawain A, a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.
体外活性	FLAVOKAVAIN A(P) significant inhibition on CYP1A2, CYP2D1, CYP2C6 and CYP3A2 activities with IC50 values of 102.23, 20.39, 69.95, 60.22μmol/L, respectively. The inhibition model was competitive, mixed-inhibition, uncompetitive, and noncompetitive for CYP1A2, CYP2D1, CYP2C6 and CYP3A2 enzymes. Molecular docking study indicated the ligand-binding conformation of FLAVOKAVAIN A(P) in the active site of CYP450 isoforms. The chemical inhibition experiments showed that the metabolic clearance rate of Flavokawain A decreased to 19.84%, 50.38%, and 67.02% of the control in the presence of ketoconazole, sulfamethoxazde and a-naphthoflavone[1].
体内活性	FLAVOKAVAIN A(P) results in a significant loss of mitochondrial membrane potential and release of cytochrome c into the cytosol in an invasive bladder cancer cell line T24. These effects of flavokawain A are accompanied by a time-dependent decrease in Bcl-x(L), a decrease in the association of Bcl-x(L) to Bax, and an increase in the active form of Bax protein. Using the primary mouse embryo fibroblasts Bax knockout and wild-type cells as well as a Bax inhibitor peptide derived from the Bax-binding domain of Ku70, Bax protein was, at least in part, required for the apoptotic effect of flavokawain A. In addition, flavokawain A down-regulates the expression of X-linked inhibitor of apoptosis and survivin. Because both X-linked inhibitor of apoptosis and survivin are main factors for apoptosis resistance and are overexpressed in bladder tumors, Suggest that flavokawain A may have a dual efficacy in induction of apoptosis preferentially in bladder tumors[2].
激酶实验	Probe-based assays with rat liver microsome system were used to characterize the inhibitory effects of FLAVOKAVAIN A(P). Molecular docking study was performed to further explore the binding site of FLAVOKAVAIN A(P) on CYP450 isoforms. Chemical inhibition experiments using specific inhibitors (a-naphthoflavone, quinidine, sulfamethoxazde, ketoconazole, omeprazole) were performed to clarify the individual CYP450 isoform that are responsible for the metabolism of FLAVOKAVAIN A(P)[1].
动物实验	Flavokawain A was formulated in 10% grain alcohol in 0.9% saline and given by gavage. EJ bladder tumor cells were concentrated to 2 × 10^6 per 200 μL and injected s.c. into the right flank of each mouse. Next day, the mice were randomly divided and pair matched into treatment and control groups of 18 mice each, and daily dosing was begun with vehicle or 50 mg/kg flavokawain A. Because there were no in vivo data regarding flavokawain A before this study, the dose of flavokawain A (50 mg/kg/d) was used according to 1:60 of 3,000 mg/kg, a LD50 dose for a similar chemical structure compound, isoliquiritigenin . Body weight, diet, and water consumption were recorded thrice weekly throughout the study. Once xenografts started growing, their sizes were measured every other day. The tumor volume was calculated by the formula: 0.5236 L1(L2)^2, where L1 is the long axis and L2 is the short axis of the tumor. At the end of experiment, tumors were excised, weighed, blood collected, and stored at ?80°C until additional analysis[2].

别名	(E)-1-(2-羟基-4,6-二甲氧基苯基)-3-(4-甲氧基苯基)-2-丙烯-1-酮, FLAVOKAVAIN A(P), 卡瓦胡椒素A
分子量	314.33
分子式	C18H18O5
CAS No.	37951-13-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 3.14 mg/mL (10 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1814 mL	15.9068 mL	31.8137 mL	79.5342 mL
	5 mM	0.6363 mL	3.1814 mL	6.3627 mL	15.9068 mL
	10 mM	0.3181 mL	1.5907 mL	3.1814 mL	7.9534 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Niu L , Ding L , Lu C , et al. Flavokawain A Inhibits Cytochrome P450 in in vitro Metabolic and Inhibitory Investigations[J]. Journal of Ethnopharmacology, 2016:S0378874116304007. 2. Zi X , Simoneau A R . Flavokawain A, a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.[J]. Cancer Research, 2005, 65(8):3479.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

(E)-Flavokawain A 37951-13-6 Apoptosis Metabolism P450 (E)-1-(2-羟基-4,6-二甲氧基苯基)-3-(4-甲氧基苯基)-2-丙烯-1-酮 inhibit Inhibitor (E) Flavokawain A FLAVOKAVAIN A(P) (E)Flavokawain A Flavokawain A 卡瓦胡椒素A inhibitor

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(E)-Flavokawain A

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

Keywords