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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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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)

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

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.

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

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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Protection by phosphodiesterase inhibitors against endotoxin-induced liver injury in galactosamine-sensitized mice.

W Fischer et al.

Biochemical pharmacology, 45(12), 2399-2404 (1993-06-22)

Phosphodiesterase inhibitors were used as a tool to manipulate cellular nucleotide levels in vitro and in vivo. The lipopolysaccharide (LPS)-induced release of tumor necrosis factor alpha (TNF-alpha) from mouse peritoneal macrophages was inhibited by prostaglandin E2 with an IC50 of

Phosphodiesterase isozymes modulating inherent tone in human airways: identification and characterization.

K F Rabe et al.

The American journal of physiology, 264(5 Pt 1), L458-L464 (1993-05-01)

The effects of the nonselective phosphodiesterase (PDE)-inhibitor 3-isobutyl-1-methylxanthine (IBMX) and the selective PDE inhibitors SKF 94120 (type III), rolipram (type IV), zardaverine (type III/IV), and zaprinast (type V) on inherent tone in human airways were investigated. Substantial relaxation was achieved

Low-dose systemic phosphodiesterase inhibitors amplify the pulmonary vasodilatory response to inhaled prostacyclin in experimental pulmonary hypertension.

R T Schermuly et al.

American journal of respiratory and critical care medicine, 160(5 Pt 1), 1500-1506 (1999-11-11)

Inhalation of aerosolized prostaglandin I(2) (PGI(2)) causes selective pulmonary vasodilation, but the effect rapidly levels off after termination of nebulization. In experimental pulmonary hypertension in intact rabbits, provoked by continuous infusion of the stable thromboxane mimetic U46619, the impact of

Targeting tumor cells based on Phosphodiesterase 3A expression.

Madiha Nazir et al.

Experimental cell research, 361(2), 308-315 (2017-11-07)

We and others have previously reported a correlation between high phosphodiesterase 3A (PDE3A) expression and selective sensitivity to phosphodiesterase (PDE) inhibitors. This indicates that PDE3A could serve both as a drug target and a biomarker of sensitivity to PDE3 inhibition.

The effect of zardaverine, an inhibitor of phosphodiesterase isoenzymes III and IV, on endotoxin-induced airway changes in rats.

J C Kips et al.

Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 23(6), 518-523 (1993-06-01)

Zardaverine is a novel phosphodiesterase III/IV inhibitor, developed as a potential therapeutic agent for asthma. In this study we evaluated the effect of zardaverine in an in vivo animal model of airway inflammation and hyperresponsiveness. Endotoxin exposure in rats causes

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Global Trade Item Number

SKU	GTIN
Z3003-5MG	04061832950099

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