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Merck
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Z3003

Sigma-Aldrich

Zardaverine

powder, ≥98% (HPLC)

Sinônimo(s):

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

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About This Item

Fórmula empírica (Notação de Hill):
C12H10F2N2O3
Número CAS:
101975-10-4
Peso molecular:
268.22
Número MDL:
MFCD00867059
Código UNSPSC:
12352202
ID de substância PubChem:
24278784
NACRES:
NA.77

product name

Zardaverine,

cadeia de caracteres SMILES

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)

chave InChI

HJMQDJPMQIHLPB-UHFFFAOYSA-N

Informações sobre genes

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

Aplicação

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

Ações bioquímicas/fisiológicas

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).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Equipamento de proteção individual

Eyeshields, Gloves, type N95 (US)

Certificados de análise (COA)

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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
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
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
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.
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)
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