Zardaverine
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MedKoo CAT#: 326721

CAS#: 101975-10-4

Description: Zardaverine is a Phosphodiesterase 3/4 inhibitor. Zardaverine exhibits potent and selective antitumor activity against hepatocellular carcinoma both in vitro and in vivo independently of phosphodiesterase inhibition. Zardaverine may be also useful for both, bronchorelaxation and reduction of inflammation in asthma therapy.

Chemical Structure

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Zardaverine
CAS# 101975-10-4
Instruction

Theoretical Analysis

MedKoo Cat#: 326721
Name: Zardaverine
CAS#: 101975-10-4
Chemical Formula: C12H10F2N2O3
Exact Mass: 268.07
Molecular Weight: 268.220
Elemental Analysis: C, 53.74; H, 3.76; F, 14.17; N, 10.44; O, 17.89

Price and Availability

Size Price Availability Quantity
5mg USD 190
10mg USD 350
25mg USD 650
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Synonym: Zardaverine

IUPAC/Chemical Name: 6-(4-(Difluoromethoxy)-3-methoxyphenyl)-3(2H)-pyridazinone

InChi Key: HJMQDJPMQIHLPB-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H10F2N2O3/c1-18-10-6-7(2-4-9(10)19-12(13)14)8-3-5-11(17)16-15-8/h2-6,12H,1H3,(H,16,17)

SMILES Code: O=C1C=CC(C2=CC=C(OC(F)F)C(OC)=C2)=NN1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 268.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Sun L, Quan H, Xie C, Wang L, Hu Y, Lou L. 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. doi: 10.1371/journal.pone.0090627. eCollection 2014. PubMed PMID: 24598942; PubMed Central PMCID: PMC3944092.

2: Schermuly RT, Leuchte H, Ghofrani HA, Weissmann N, Rose F, Kohstall M, Olschewski H, Schudt C, Grimminger F, Seeger W, Walmrath D. Zardaverine and aerosolised iloprost in a model of acute respiratory failure. Eur Respir J. 2003 Aug;22(2):342-7. PubMed PMID: 12952271.

3: Ukena D, Rentz K, Reiber C, Sybrecht GW. Effects of the mixed phosphodiesterase III/IV inhibitor, zardaverine, on airway function in patients with chronic airflow obstruction. Respir Med. 1995 Jul;89(6):441-4. PubMed PMID: 7644776.

4: Hoymann HG, Heinrich U, Beume R, Kilian U. Comparative investigation of the effects of zardaverine and theophylline on pulmonary function in rats. Exp Lung Res. 1994 May-Jun;20(3):235-50. PubMed PMID: 7925141.

5: Kips JC, Joos GF, Peleman RA, Pauwels RA. 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. PubMed PMID: 8369979.

6: Schade FU, Schudt C. The specific type III and IV phosphodiesterase inhibitor zardaverine suppresses formation of tumor necrosis factor by macrophages. Eur J Pharmacol. 1993 Jan 5;230(1):9-14. PubMed PMID: 8381357.

7: Brunnée T, Engelstätter R, Steinijans VW, Kunkel G. Bronchodilatory effect of inhaled zardaverine, a phosphodiesterase III and IV inhibitor, in patients with asthma. Eur Respir J. 1992 Sep;5(8):982-5. PubMed PMID: 1426207.

8: Huber R, Schildnitz U. 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. J Chromatogr. 1991 Aug 16;553(1-2):65-70. PubMed PMID: 1787170.

9: Schudt C, Winder S, Müller B, Ukena D. Zardaverine as a selective inhibitor of phosphodiesterase isozymes. Biochem Pharmacol. 1991 Jun 21;42(1):153-62. PubMed PMID: 1648920.

10: Schudt C, Winder S, Eltze M, Kilian U, Beume R. Zardaverine: a cyclic AMP specific PDE III/IV inhibitor. Agents Actions Suppl. 1991;34:379-402. Review. PubMed PMID: 1665311.

11: Galvan M, Schudt C. Actions of the phosphodiesterase inhibitor zardaverine on guinea-pig ventricular muscle. Naunyn Schmiedebergs Arch Pharmacol. 1990 Aug;342(2):221-7. PubMed PMID: 1700309.