货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V52786-1ml	10mM in DMSO	￥900.00 V52786-1ml ￥900.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V52786-1ml

10mM in DMSO

￥900.00

货期：3-5天

产品描述：

Siguazodan (SKF 94836) 是一种有效的，选择性的，口服活性的磷酸二酯酶 III (PDE-III) 抑制剂，IC50 为 117 nM。Siguazodan 可增加完整血小板中 cAMP 的积累，EC50 为 18.88 μM。Siguazodan 还抑制苯肾上腺素诱导的 5-HT 释放，IC50 值为 4.2 μM。

靶点：

IC50: 117 nM (phosphodiesterase III)

体外研究：

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.

体内研究：

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.

参考文献：

1. Tang KM, et al. Photoaffinity labelling of cyclic GMP-inhibited phosphodiesterase (PDE III) in human and rat platelets and rat tissues: effects of phosphodiesterase inhibitors. Eur J Pharmacol. 1994 Jun 15;268(1):105-14.

2. Murray KJ, et al. The effects of siguazodan, a selective phosphodiesterase inhibitor, on human platelet function. Br J Pharmacol. 1990 Mar;99(3):612-6.

3. Freitag A, et al. Phosphodiesterase inhibitors suppress alpha2-adrenoceptor-mediated 5-hydroxytryptamine release from tracheae of newborn rabbits. Eur J Pharmacol. 1998 Jul 31;354(1):67-71.

溶解性：

soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.517 ml	17.586 ml	35.172 ml
5 mM	0.703 ml	3.517 ml	7.034 ml
10 mM	0.352 ml	1.759 ml	3.517 ml
50 mM	0.07 ml	0.352 ml	0.703 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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