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Zardaverine CAS: 101975-10-4

Category: Inhibitors
Product Name: Zardaverine
Cat No: I000141
CAS No: 101975-10-4
Synonyms: 6-(4-(difluoromethoxy)-3-methoxyphenyl)pyridazin-3(2H)-one
Molecular Formula: C12H10F2N2O3
Molecular Weight: 268.22
SMILES: O=C1C=CC(C2=CC=C(OC(F)F)C(OC)=C2)=NN1
InChI: None
InChIKey: None
Solubility: DMSO: ≥ 28 mg/mL
Target: PDE
IC50: 0.5 uM (PDE3); 0.8 uM (PDE4)
Storage: Store at -20°C
CAS 101975-10-4,Zardaverine
  • Description

Zardaverine is a newly developed dual-selective PDE3/4 inhibitor with IC50 values of 0.5 uM and 0.8 uM respectively.
IC50 value: 0.5 uM (PDE3); 0.8 uM (PDE4)
Target: PDE3; PDE4
Zardaverine inhibited the cyclic GMP-inhibitable PDE III from human platelets and the rolipram-inhibitable PDE IV from canine trachea and human polymorphonuclear (PMN) cells with IC50-values of 0.58, 0.79 and 0.17 μM, respectively. The pyridazinone derivative affected the calmodulin-stimulated PDE I, the cyclic GMP-stimulated PDE II and the cyclic GMP-specific PDE V only marginally at concentrations up to 100μM. Zardaverine inhibits the ADP-induced aggregation of human platelets with an IC50 of 1.6 μM. This inhibition was synergistically increased by activators of adenylate cyclase such as PGE1 and forskolin. In human PMN cells, Zardaverine inhibited the zymosan-induced superoxide anion generation with an IC50 of 0.40 μM. Again, this effect was increased by activators of adenylate cyclase. Zardaverine acted in synergy with the adenylate cyclase activators prostaglandin E2 and CG 4203, a prostacyclin analog, and super-additive effects of combinations were observed. Zardaverine and dexamethasone prevent bronchial eosinophilia and neutrophilia with similar dosage of 30 microM/kg orally, suggesting that this PDE III/IV inhibitor may be useful for both, bronchorelaxation and reduction of inflammation in asthma therapy.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Cytotoxicity of Zardaverine in Embryonal Rhabdomyosarcoma from a Costello Syndrome Patient. Cartledge DM, Robbins KM, Drake KM, Sternberg R, Stabley DL, Gripp KW, Kolb EA, Sol-Church K, Napper AD.Front Oncol. 2017 Apr 3;7:42. doi: 10.3389/fonc.2017.00042. eCollection 2017. PMID: 28421158 Free PMC Article
2:Phosphodiesterase 3/4 inhibitor zardaverine exhibits potent and selective antitumor activity against hepatocellular carcinoma both in vitro and in vivo independently of phosphodiesterase inhibition. Sun L, Quan H, Xie C, Wang L, Hu Y, Lou L.PLoS One. 2014 Mar 5;9(3):e90627. doi: 10.1371/journal.pone.0090627. eCollection 2014. PMID: 24598942 Free PMC Article
3:Zardaverine and aerosolised iloprost in a model of acute respiratory failure. Schermuly RT, Leuchte H, Ghofrani HA, Weissmann N, Rose F, Kohstall M, Olschewski H, Schudt C, Grimminger F, Seeger W, Walmrath D.Eur Respir J. 2003 Aug;22(2):342-7. PMID: 12952271 Free Article
4:Effects of the mixed phosphodiesterase III/IV inhibitor, zardaverine, on airway function in patients with chronic airflow obstruction. Ukena D, Rentz K, Reiber C, Sybrecht GW.Respir Med. 1995 Jul;89(6):441-4. PMID: 7644776 Free Article
5:Comparative investigation of the effects of zardaverine and theophylline on pulmonary function in rats. Hoymann HG, Heinrich U, Beume R, Kilian U.Exp Lung Res. 1994 May-Jun;20(3):235-50. PMID: 7925141
6:The effect of zardaverine, an inhibitor of phosphodiesterase isoenzymes III and IV, on endotoxin-induced airway changes in rats. Kips JC, Joos GF, Peleman RA, Pauwels RA.Clin Exp Allergy. 1993 Jun;23(6):518-23. PMID: 8369979
7:The specific type III and IV phosphodiesterase inhibitor zardaverine suppresses formation of tumor necrosis factor by macrophages. Schade FU, Schudt C.Eur J Pharmacol. 1993 Jan 5;230(1):9-14. PMID: 8381357
8:Bronchodilatory effect of inhaled zardaverine, a phosphodiesterase III and IV inhibitor, in patients with asthma. Brunnée T, Engelstätter R, Steinijans VW, Kunkel G.Eur Respir J. 1992 Sep;5(8):982-5. PMID: 1426207
9:Sensitive determination of the phosphodiesterase III/IV inhibitor zardaverine in human serum by direct sample injection, automated precolumn clean-up and high-performance liquid chromatography. Huber R, Schildnitz U.J Chromatogr. 1991 Aug 16;553(1-2):65-70. PMID: 1787170
10:Zardaverine as a selective inhibitor of phosphodiesterase isozymes. Schudt C, Winder S, Müller B, Ukena D.Biochem Pharmacol. 1991 Jun 21;42(1):153-62. PMID: 1648920


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