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

Zardaverine 

Cat. No.: HY-15485 Purity: 98.73%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Zardaverine Chemical Structure

Zardaverine Chemical Structure

CAS No. : 101975-10-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 90 In-stock
50 mg USD 360 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].

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].

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

Appearance

Solid

Formula

C12H10F2N2O3
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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
10 mM 0.3728 mL 1.8641 mL 3.7283 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.73%

COA (251 KB) HNMR (261 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
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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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Keywords:

Zardaverine101975-10-4Phosphodiesterase (PDE)ApoptosisHCCasthmabronchodilatorBel-7402Bel-7404QGY-7701SMMC-7721cancerhepatocellular carcinomaInhibitorinhibitorinhibit

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