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Zardaverine
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。
Zardaverine图片
CAS NO:101975-10-4
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
扎达维林
产品介绍
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。
生物活性

Zardaverine is an orally active and selectivePDE3/4inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and inducesapoptosisand 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].

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.

Cell Cycle Analysis[1]

Cell Line:Bel-7402, Bel-7404, QGY-7701 and SMMC-7721
Concentration:0.1 μM
Incubation Time:24 h
Result:Induced accumulation of Bel-7402, Bel-7404, QGY-7701 and SMMC-7721 cells in the G0/G1 phase.

Western Blot Analysis[1]

Cell Line:Bel-7402, SMMC-7721
Concentration:0.01, 0.03, 0.1, 0.3 1 μM; 0.3 1 μM
Incubation Time:48 h; 24, 36, 48, 60, 72 h
Result:Induced a concentration- and time- dependent increase in the cleavage of PARP and caspase-3, -8 and -9, which are apoptosis markers.
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].

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.
Animal Model:Inbred male Fisher 344 (F344) rats (250-350 g; 3 to 4-month-old; airway inflammation and hyperresponsiveness model)[2].
Dosage:8046.6 μg/kg (30 μmol/Kg)
Administration:Intraperitoneal injection; single
Result:Completely blocked LPS-induced hyperresponsiveness and airway inflammation.
分子量

268.22

性状

Solid

Formula

C12H10F2N2O3

CAS 号

101975-10-4

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°C6 months
-20°C1 month
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℃, 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。

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

    此方案可获得 ≥ 2.08 mg/mL (7.75 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
  • 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

    此方案可获得 ≥ 2.08 mg/mL (7.75 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在本网站选购。