| Description | RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1]. |
| Synonyms | CAY10441 |
| molecular weight | 309.41 |
| Molecular formula | C19H23N3O |
| CAS | 221529-58-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (145.44 mM) |
| References | 1. Clark R D, Jahangir A, Severance D, et al. Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists[J]. Bioorganic & medicinal chemistry letters, 2004, 14(4): 1053-1056. |