Z3003
Zardaverine
powder, ≥98% (HPLC)
别名:
6-(4-Difluoromethoxy-3-methoxyphenyl)-3(2H)-pyridazinone
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关于此项目
经验公式（希尔记法）:
C12H10F2N2O3
化学文摘社编号:
分子量:
268.22
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
Zardaverine,
Quality Level
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
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).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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
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
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
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| Z3003-5MG | 04061832950099 |
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