CAY10449

Recently, a series of relatively simple compounds were found to be high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor. CAY10449 is one of the more potent of these. CAY10449 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 value of about 3 nM. Although CAY10449 was not tested in rats, the related compound CAY10441 shows significant analgesic activity in standard antinociceptive assays.Formal Name: 4,5-dihydro-N-[4-[[4-(1-methylethoxy)phenyl]carbonyl]phenyl]-1H-imadazol-2-amine. Molecular Formula: C19H21N3O2. Formula Weight: 323.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMF:PBS (pH 7.2)(1:1): .5 mg/ml, DMSO: 2 mg/ml. lambdamax: 227, 299 nm. SMILES: CC(C)Oc1ccc(cc1)C(=O)c1ccc(cc1)NC1=NCCN1. InChi Code: InChI=1S/C19H21N3O2/c1-13(2)24-17-9-5-15(6-10-17)18(23)14-3-7-16(8-4-14)22-19-20-11-12-21-19/h3-10,13H,11-12H2,1-2H3,(H2,20,21,22). InChi Key: SPGYSLWXEKMJAN-UHFFFAOYSA-N.