1. Metabolic Enzyme/Protease Apoptosis
  2. Phosphodiesterase (PDE) Apoptosis
  3. Zardaverine

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.

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Zardaverine Chemical Structure

Zardaverine Chemical Structure

CAS No. : 101975-10-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 90 In-stock
50 mg USD 288 In-stock
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Description

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

 

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].

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

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.
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].

MedChemExpress (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.
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.
Molecular Weight

268.22

Formula

C12H10F2N2O3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1C=CC(C2=CC=C(OC(F)F)C(OC)=C2)=NN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (93.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7283 mL 18.6414 mL 37.2828 mL
5 mM 0.7457 mL 3.7283 mL 7.4566 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.73%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7283 mL 18.6414 mL 37.2828 mL 93.2071 mL
5 mM 0.7457 mL 3.7283 mL 7.4566 mL 18.6414 mL
10 mM 0.3728 mL 1.8641 mL 3.7283 mL 9.3207 mL
15 mM 0.2486 mL 1.2428 mL 2.4855 mL 6.2138 mL
20 mM 0.1864 mL 0.9321 mL 1.8641 mL 4.6604 mL
25 mM 0.1491 mL 0.7457 mL 1.4913 mL 3.7283 mL
30 mM 0.1243 mL 0.6214 mL 1.2428 mL 3.1069 mL
40 mM 0.0932 mL 0.4660 mL 0.9321 mL 2.3302 mL
50 mM 0.0746 mL 0.3728 mL 0.7457 mL 1.8641 mL
60 mM 0.0621 mL 0.3107 mL 0.6214 mL 1.5535 mL
80 mM 0.0466 mL 0.2330 mL 0.4660 mL 1.1651 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Zardaverine
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