Ro-15-2041

Ro15-2041是选择性血小板磷酸二酯酶抑制剂,具有抗血栓性质。

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库存: 现货

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1mg

￥8350.00

6680.00

- +
5mg

￥16525.00

13220.00

- +
10mg

￥28075.00

22460.00

- +
20mg

￥49587.00

39670.00

- +

已选 0 种 0 瓶

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Background

Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.

Ro 15-2041 inhibits platelet aggregation induced by all common platelet agonists in platelet-rich plasma obtained from various species including man (IC50=1-3 μM). Ro 15-2041 potentiates platelet inhibition by prostacyclin, the prostacyclin-induced increase of intraplatelet cyclic (c) AMP levels and inhibits the collagen-induced release of serotonin and beta-thromboglobulin. Ro 15-2041 reduces the increase and accelerated the normalization of cytosolic free Ca2+ in thrombin-stimulated human platelets. Ro 15-2041 is a potent (IC50=70 nM) and selective inhibitor of platelet cAMP-phosphodiesterase activity. Whereas Ro 15-2041 causes complete inhibition of cAMP-phosphodiesterase activity in human platelet supernatants, breakdown of cAMP in cardiac homogenates is depressed to maximally 50%. In human brain and rabbit uterus Ro 15-2041 is at least 1000 times less potent. By comparison, papaverine fully inhibits phosphodiesterase activity in all four tissues with similar IC50 values of about 5 μM. Furthermore, Ro 15-2041 selectively inhibits cAMP-phosphodiesterase activity of a bovine calmodulin-independent but not of a calmodulin-dependent enzyme preparation[1].

[1]. Muggli R, et al. 7-Bromo-1,5-dihydro-3,6-dimethylimidazo[2,1-b]quinazolin-2(3H)- one (Ro 15-2041), a potent antithrombotic agent that selectively inhibits platelet cyclic AMP-phosphodiesterase. J Pharmacol Exp Ther. 1985 Oct;235(1):212-9.