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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)

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This Item	C7971	SRP0262	SRP0429
Sigma-Aldrich Z3003 Zardaverine	Sigma-Aldrich C7971 Cilostamide	Sigma-Aldrich SRP0262 PDE4A1A Active human	Sigma-Aldrich SRP0429 PDE4A10 active human
Gene Information human ... PDE3A(5139), PDE3B(5140), PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144), PDE5A(8654), PDE7A(5150) rat ... Pde2a(81743), Pde4a(25638)	Gene Information human ... PDE3A(5139), PDE3B(5140), PDE5A(8654), PDE7A(5150) rat ... Pde2a(81743), Pde4a(25638)	Gene Information human ... PDE4A(5141)	Gene Information human ... PDE4A(5141)
Quality Level 200	Quality Level 100	Quality Level -	Quality Level -

Application

Zardaverine has been used as a phosphodiesterase inhibitor:

to study its effects on human colonic epithelial cells[1]
to study its effects on junctional proteins in Sertoli cells[2]
to study its effects on phosphodiesterase 3 A (PDE3A) expression in various tumor cells[3]

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.[3]

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

Differential effects of non-selective and selective phosphodiesterase inhibitors on human eosinophil functions.

A Hatzelmann et al.

British journal of pharmacology, 114(4), 821-831 (1995-02-01)

1. The effect of non-selective (3-isobutyl-1-methylxanthine, IBMX; theophylline) and type IV- or type III/IV-selective (rolipram, RP 73401; zardaverine, tolafentrine) phosphodiesterase (PDE) inhibitors on human eosinophil functions was investigated. 2. For this purpose human eosinophils were purified from blood of healthy

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

Bronchodilator and positive inotropic activity of pyridazine compound Zardaverine as a phosphodiesterase isozymes inhibitor

Asif M

Journal of Chemical and Pharmaceutical Sciences , 3(1), 31-34 null

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.

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Global Trade Item Number

SKU	GTIN
Z3003-5MG	04061832950099

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