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Ro-15-2041 Sale

目录号 : GC32555

Ro15-2041是选择性血小板磷酸二酯酶抑制剂,具有抗血栓性质。

Ro-15-2041 Chemical Structure

Cas No.:77448-87-4

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1mg
¥6,962.00
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5mg
¥13,923.00
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10mg
¥23,651.00
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20mg
¥41,769.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

Cas No. 77448-87-4 SDF
Canonical SMILES O=C1N=C2NC3=C(C(C)=C(Br)C=C3)CN2C1C
分子式 C12H12BrN3O 分子量 294.15
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.3996 mL 16.9981 mL 33.9963 mL
5 mM 0.6799 mL 3.3996 mL 6.7993 mL
10 mM 0.34 mL 1.6998 mL 3.3996 mL
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