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.
For research use only. We do not sell to patients.
- Purity : 98.59%
- CAS No.: 101975-10-4
- Formula: C12H10F2N2O3
- Molecular Weight:268.22
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-14252
Milrinone -
HY-15455
RoflumilastPDE4 Inhibitor -
HY-B0204
PimobendanPDE Inhibitor -
HY-101312
CilostamidePDE3 Inhibitor -
HY-B0312
DipyridamolePDE Inhibitor -
HY-100927
Ro 20-1724PDE4/PDE IV Inhibitor -
HY-10790
CilomilastPDE4 Inhibitor -
HY-14254
Olprinone HydrochloridePhosphodiesterase 3 Inhibitor -
HY-B1639
EnoximonePDE3 Inhibitor -
HY-16900
RolipramPDE4 Inhibitor -
HY-10469
GSK256066Phosphodiesterase 4 Inhibitor -
HY-12085
ApremilastPDE-4 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Zardaverine
More
Biological Activity
Description
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. Further protocols information, click here.
-
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 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.
-
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 (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.
Chemical Information
-
CAS No. 101975-10-4
-
Appearance Solid
-
Molecular Weight 268.22
-
Formula C12H10F2N2O3
-
Color White to 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
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
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
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)
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)
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protocols
-
Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
-
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
-
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
-
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
-
Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
-
Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
-
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
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
Powered by Bioz