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Z3003

Sigma-Aldrich

Zardaverine

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
MDL number:
MFCD00867059
UNSPSC Code:
12352202
PubChem Substance ID:
24278784
NACRES:
NA.77

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

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

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Certificates of Analysis (COA)

Lot/Batch Number
SLCR4833
SLCD6156
SLCC9883
SLCC0064
SLBZ8251

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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.
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
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.
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
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
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