77448-87-4
77448-87-4 structure
- Name: Ro-15-2041
- Chemical Name: Ro-15-2041
- CAS Number: 77448-87-4
- Molecular Formula: C12H12BrN3O
- Molecular Weight: 294.147
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
- Create Date: 2018-06-09 22:21:03
- Modify Date: 2024-02-28 22:17:47
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Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
| Name | Ro-15-2041 |
|---|---|
| Synonyms |
Imidazo[2,1-b]quinazolin-2(3H)-one, 7-bromo-5,10-dihydro-3,6-dimethyl-
7-Bromo-3,6-dimethyl-5,10-dihydroimidazo[2,1-b]quinazolin-2(3H)-one 7-Bromo-1,5-dihydro-3,6-dimethylimidazo(2,1-b)quinazolin-2(3H)-one |
| Description | Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties. |
|---|---|
| Related Catalog | |
| Target |
phosphodiesterase[1] |
| 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[1]. |
| References |
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Boiling Point | 375.8±52.0 °C at 760 mmHg |
| Molecular Formula | C12H12BrN3O |
| Molecular Weight | 294.147 |
| Flash Point | 181.1±30.7 °C |
| Exact Mass | 293.016357 |
| LogP | 2.18 |
| Vapour Pressure | 0.0±0.9 mmHg at 25°C |
| Index of Refraction | 1.744 |
| Storage condition | 2-8℃ |