Zardaverine
Based on 1 publication(s) in Google Scholar
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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- Purity: 98.59%
- CAS No.: 101975-10-4
- 화학식: C12H10F2N2O3
- 분자량:268.22
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Zardaverine
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Biological Activity
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PDE3 |
PDE4 |
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.
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Cell Line:Bel-7402, Bel-7404, QGY-7701 and SMMC-7721
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Concentration:0-30 µM
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Incubation Time:72 h
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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.
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Cell Line:Bel-7402, Bel-7404, QGY-7701 and SMMC-7721
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Concentration:0.1 µM
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Incubation Time:24 h
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Result:Induced accumulation of Bel-7402, Bel-7404, QGY-7701 and SMMC-7721 cells in the G0/G1 phase.
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Cell Line:Bel-7402, SMMC-7721
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Concentration:0.01, 0.03, 0.1, 0.3 1 µM; 0.3 1 µM
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Incubation Time:48 h; 24, 36, 48, 60, 72 h
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Result:Induced a concentration- and time- dependent increase in the cleavage of PARP and caspase-3, -8 and -9, which are apoptosis markers.
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.
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Animal Model:Female Balb/cA-nude mice (5 to 6-week-old; human Bel-7402 xenografts model)[1].
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Dosage:60, 200 mg/kg
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Administration:Oral administration; single daily for 14 days
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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.
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Animal Model:Inbred male Fisher 344 (F344) rats (250-350 g; 3 to 4-month-old; airway inflammation and hyperresponsiveness model)[2].
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Dosage:8046.6 µg/kg (30 µmol/Kg)
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Administration:Intraperitoneal injection; single
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Result:Completely blocked LPS-induced hyperresponsiveness and airway inflammation.
Chemical Information
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CAS No. 101975-10-4
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Appearance Solid
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분자량 268.22
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화학식 C12H10F2N2O3
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Color White to yellow
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SMILES
O=C1C=CC(C2=CC=C(OC(F)F)C(OC)=C2)=NN1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Toxicol Lett
Discovery of non-steroidal aldo-keto reductase 1D1 inhibitors through automated screening and in vitro evaluation. [Abstract]2025 Apr:406:31-37. PMID: 39988211
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
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- Deutsch - DE (396 KB)
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- Español - ES (396 KB)
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- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Sun L, et al. Phosphodiesterase 3/4 inhibitor zardaverine exhibits potent and selective antitumor activity against hepatocellular carcinoma both in vitro and in vivo independently of phosphodiesterase inhibition. PLoS One. 2014 Mar 5;9(3):e90627. [Content Brief]
[2]. Kips JC, et al. The effect of zardaverine, an inhibitor of phosphodiesterase isoenzymes III and IV, on endotoxin-induced airway changes in rats. Clin Exp Allergy. 1993 Jun;23(6):518-23. [Content Brief]
[3]. Schudt C, et al. Zardaverine: a cyclic AMP specific PDE III/IV inhibitor. Agents Actions Suppl. 1991;34:379-402. [Content Brief]
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 |
Zardaverine Related Classifications
HY-15485 Related Classifications
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