Ro-15-2041 

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

phosphodiesterase^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

294.15

C₁₂H₁₂BrN₃O

77448-87-4

O=C1N=C2NC3=C(C(C)=C(Br)C=C3)CN2C1C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]