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Z3003

Zardaverine

Name: Zardaverine
Brand: SIGMA

powder, ≥98% (HPLC)

Synonym(s):

6-(4-Difluoromethoxy-3-methoxyphenyl)-3(2H)-pyridazinone

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About This Item

Empirical Formula (Hill Notation):

C₁₂H₁₀F₂N₂O₃

CAS Number:

101975-10-4

Molecular Weight:

268.22

UNSPSC Code:

12352202

PubChem Substance ID:

24278784

NACRES:

NA.77

MDL number:

MFCD00867059

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Properties

Product Name

Zardaverine,

Quality Level

200

SMILES string

COc1cc(ccc1OC(F)F)C2=NNC(=O)C=C2

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)

InChI key

HJMQDJPMQIHLPB-UHFFFAOYSA-N

Gene Information

human ... PDE3A(5139), PDE3B(5140), PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144), PDE5A(8654), PDE7A(5150)
rat ... Pde2a(81743), Pde4a(25638)

Description

Application

Zardaverine has been used as a phosphodiesterase inhibitor:

to study its effects on human colonic epithelial cells
to study its effects on junctional proteins in Sertoli cells
to study its effects on phosphodiesterase 3 A (PDE3A) expression in various tumor cells

Biochem/physiol Actions

Selective inhibitor of phosphodiesterase III/IV (PDE3/4).

Zardaverine is a derivative of pyridazinone. It shows anti-tumor and anti-proliferative activity in varied cell lines. Zardaverine possesses broncho-dilatory activity and exhibits therapeutic effects against asthma.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Suppression of human eosinophil respiratory burst and cyclic AMP hydrolysis by inhibitors of type IV phosphodiesterase: interaction with the beta adrenoceptor agonist albuterol.

G Dent et al.

The Journal of pharmacology and experimental therapeutics, 271(3), 1167-1174 (1994-12-01)

The cyclic AMP phosphodiesterase (PDE) III/IV inhibitor, zardaverine, and the PDE IV-selective inhibitor, rolipram, both caused concentration-dependent inhibition of opsonized zymosan-stimulated superoxide anion generation by purified human peripheral blood eosinophils with approximate IC50 values of 30 and 40 microM, respectively.

Bronchodilatory effect of inhaled zardaverine, a phosphodiesterase III and IV inhibitor, in patients with asthma.

T Brunnée et al.

The European respiratory journal, 5(8), 982-985 (1992-09-01)

Zardaverine is a newly developed selective phosphodiesterase III and IV inhibitor. This study investigates the bronchodilatory properties of zardaverine, administered by inhalation. Twelve patients with reversible bronchial obstruction (increase in forced expiratory volume in one second (change FEV1 % predicted)

Evidence that the anti-spasmogenic effect of the beta-adrenoceptor agonist, isoprenaline, on guinea-pig trachealis is not mediated by cyclic AMP-dependent protein kinase.

L Spicuzza et al.

British journal of pharmacology, 133(8), 1201-1212 (2001-08-11)

1. The spasmolytic and anti-spasmogenic activity of beta-adrenoceptor agonists on airways smooth muscle is thought to involve activation of the cyclic AMP/cyclic AMP-dependent protein kinase (PKA) cascade. Here we have tested the hypothesis that PKA mediates the anti-spasmogenic activity of

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Global Trade Item Number

SKU	GTIN
Z3003-5MG	04061832950099