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Z3003

Sigma-Aldrich

Zardaverine

powder, ≥98% (HPLC)

Synonym(e):

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

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About This Item

Empirische Formel (Hill-System):
C12H10F2N2O3
CAS-Nummer:
101975-10-4
Molekulargewicht:
268.22
MDL-Nummer:
MFCD00867059
UNSPSC-Code:
12352202
PubChem Substanz-ID:
24278784
NACRES:
NA.77

product name

Zardaverine,

Qualitätsniveau

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)

InChIKey

HJMQDJPMQIHLPB-UHFFFAOYSA-N

Angaben zum Gen

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

Anwendung

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. Wirkung

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).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

Eyeshields, Gloves, type N95 (US)

Analysenzertifikate (COA)

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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
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
D T Schmidt et al.
British journal of pharmacology, 131(8), 1607-1618 (2001-01-05)
Non-selective inhibitors of cyclic nucleotide phosphodiesterase (PDE) block allergen-induced contraction of passively sensitized human airways in vitro by a dual mechanism involving a direct relaxant effect on smooth muscle and inhibition of histamine and cysteinyl leukotriene (LT) release from airways.
K F Rabe et al.
The American journal of physiology, 266(5 Pt 1), L536-L543 (1994-05-01)
The effects of the nonselective phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine (IBMX) and the selective PDE inhibitors motapizone (type III), rolipram (type IV), zardaverine (type III/IV), and zaprinast (type V and I) on prostaglandin F2 alpha (PFG2 alpha)-induced tone in human pulmonary
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
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