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Zardaverine (Synonyms: 扎达维林)

Zardaverine (Synonyms: 扎达维林)

Zardaverine (Synonyms: 扎达维林)
产品编号：HY-15485
分类：分子生物学
品牌：MCE
规格：5mg
单价： ￥770.00

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Zardaverine是一种口服有效的和具有选择性的 PDE3/4 抑制剂 (IC50)=0.58 uM/0.17 uM)，具有强大的支气管扩张活性。Zardaverine 还可选择性地抑制 HCC 细胞增殖，并诱导细胞凋亡和周期停滞 (G0/G1 期)。Zardaverine 具有较好的抗肿瘤潜力，并且在哮喘中的支气管松弛和减少炎症方面均有效。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma[1][2][3].

IC50 & Target

PDE3

PDE4

体外研究
(In Vitro)

Zardaverine (0-30 µM; 72 h) selectively inhibits the growth of human HCC cells in vitro[1].
Zardaverine shows selective antitumor activity that closely related to the regulation of cell cycle-associated proteins, but is independent of PDE3/4 inhibition[1].
Zardaverine (0.1 µM; 24 h) selectively causes G0/G1-phase arrest and dysregulates cell cycle-associated proteins in HCC cells[1].
Zardaverine (0.01, 0.03, 0.1, 0.3 1 µM/48h; 0.3 1 µM/24, 36, 48, 60, 72 h) induces apoptosis in a time- and concentration- dependent manner, in Bel-7402 and SMMC-7721 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Zardaverine 相关抗体:

Cell Proliferation Assay[1]

Cell Line:Bel-7402, Bel-7404, QGY-7701 and SMMC-7721
Concentration:0-30 µM
Incubation Time:72 h
Result:Selectively inhibited SMMC-7721, QGY-7701, Bel-7402 and Bel-7404 growth with IC50s of 36.6, 51.0, 137.7 and 288.0, respectively.
体内研究
(In Vivo)

Zardaverine (60, 200 mg/kg; p.o.; single daily for 14 days) inhibits the growth of human Bel-7402 xenografts in mice[1].
Zardaverine (8046.6 µg/kg; i.p.; single) blocks the LPS induced increase in responsiveness completely in airway inflammation and hyperresponsiveness rat model[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:Female Balb/cA-nude mice (5 to 6-week-old; human Bel-7402 xenografts model)[1].
Dosage:60, 200 mg/kg
Administration:Oral administration; single daily for 14 days
Result:Inhibited the growth of Bel-7402 xenografts at the dose of 60 mg/kg for 14 consecutive days and caused the tumor regression at the dose of 200 mg/kg.
分子量

268.22

性状

Solid

Formula

C12H10F2N2O3

CAS 号
中文名称

扎达维林

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°C2 years
-20°C1 year
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (93.21 mM; Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.7283 mL18.6414 mL37.2828 mL
5 mM0.7457 mL3.7283 mL7.4566 mL
10 mM0.3728 mL1.8641 mL3.7283 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℃, 2 years; -20℃, 1 year。-80℃ 储存时，请在 2 年内使用， -20℃ 储存时，请在 1 年 内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.75 mM); Clear solution

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.75 mM); Clear solution

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