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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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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[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).

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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 -

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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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

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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