Description
Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
Product information
CAS Number: 77448-87-4
Molecular Weight: 294.15
Formula: C12H12BrN3O
Chemical Name: 7-bromo-3,6-dimethyl-2H,3H,5H,10H-imidazo[2,1-b]quinazolin-2-one
Smiles: CC1C2CN3C(C)C(=O)N=C3NC=2C=CC=1Br
InChiKey: IASFSCWLFJGXQL-UHFFFAOYSA-N
InChi: InChI=1S/C12H12BrN3O/c1-6-8-5-16-7(2)11(17)15-12(16)14-10(8)4-3-9(6)13/h3-4,7H,5H2,1-2H3,(H,14,15,17)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
Products are for research use only. Not for human use.
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