115344-47-3
基本信息
SIGUAZODAN
SK AND F-94836
Siguazodan (SKF 94836)
N-Cyano-Nmethyl-Nⅱ-[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]guanidine
N-CYANO-N'-METHYL-N''-[4-(1,4,5,6-TETRAHYDRO-4-METHYL-6-OXO-3-PYRIDAZINYL)PHENYL]GUANIDINE
Guanidine, N-cyano-N'-methyl-N''-[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]-
4β-Methyl-4,5-dihydro-3-[4-[[(cyanoimino)(methylamino)methyl]amino]phenyl]pyridazin-6(1H)-one
Siguazodan, N-Cyano-Nμ-methyl-N-[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]guanidine
[4S,(+)]-4,5-Dihydro-3-[4-[[(cyanoimino)(methylamino)methyl]amino]phenyl]-4-methylpyridazin-6(1H)-one
物理化学性质
| 熔点 | 268-268.9 °C(lit.) |
| 密度 | 1.31±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO: >5 mg/mL, freely soluble |
| 酸度系数(pKa) | 13.71±0.60(Predicted) |
| 形态 | solid |
| 颜色 | white |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H319-H335-H315 |
| 防范说明 | P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362 |
| 危险品标志 | Xi |
| 危险类别码 | 36/37/38 |
| 安全说明 | 26-36 |
| WGK Germany | 3 |
常见问题列表
IC50: 117 nM (phosphodiesterase III)
Siguazodan selectively inhibits the major cyclic AMP-hydrolysing PDE in human platelet supernatants. The inhibited enzyme has been variously termed cyclic GMP-inhibited PDE or PDE-III. In platelet-rich plasma (PRP), Siguazodan inhibits U46619-induced aggregation more potently than that induced by adenosine 5'-diphosphate (ADP), and collagen. Treatment of the PRP with Aspirin has no effect on the potency of Siguazodan. In washed platelets, Siguazodan increases cyclic AMP levels and reduces cytoplasmic free calcium. ADP decreases the ability of Siguazodan to raise cyclic AMP and this may explain its lower potency in inhibiting responses to ADP. Siguazodan has anti-platelet actions over the same concentration range that it is an inotrope and vasodilator.
Siguazodan is a potent, selective inhibitor of phosphodiesterase III that has positive inotropic and vasodilating actions in various laboratory animals and is orally active with a long duration of action in conscious dogs.