| Description | Octimibate (Octimibato) is a non-prostaglandin platelet aggregation inhibitor and cyclic prostaglandin agonist.Octimibate is used in the treatment of cardiovascular disease and can be used to study atherosclerosis and thrombosis. |
| In vitro | In suspensions of washed (plasma-free) human platelets, octimibate is a potent inhibitor of aggregation; its IC50 is approx 10 nM for inhibition of aggregation is stimulated by several different agonists, including U46619 and ADP. The inhibitory effects of octimibate on aggregation are not competitive with the stimulatory agonist; the maximal response is suppressed but there is no obvious shift in potency of the agonist. In platelet-rich plasma, octimibate inhibits agonist-stimulated aggregation with an IC50 of approx 200 nM.[2] Octimibate increases cyclic AMP concentrations in platelets and increases the cyclic AMP-dependent protein kinase activity ratio. Octimibate stimulates adenylyl cyclase activity in human platelet membranes, with an EC50 of 200 nM. The maximal achievable activation of adenylyl cyclase by intimidate is 60% of that obtainable with iloprost. Octimibate has no effect on the cyclic GMP-inhibited phosphodiesterase (phosphodiesterase-ITI), which is the major cyclic AMP-degrading enzyme in human platelets.[2] |
| Synonyms | Octimibato |
| molecular weight | 454.56 |
| Molecular formula | C29H30N2O3 |
| CAS | 89838-96-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (110 mM) |
| References | 1. Merritt JE, et al. Primate vascular responses to octimibate, a non-prostanoid agonist at the prostacyclin receptor. Br J Pharmacol. 1991;102(1):260-266. 2. Merritt JE, et al. Octimibate, a potent non-prostanoid inhibitor of platelet aggregation, acts via the prostacyclin receptor. Br J Pharmacol. 1991;102(1):251-259. 3. Seiler S, et al. Octimibate inhibition of platelet aggregation: stimulation of adenylate cyclase through prostacyclin receptor activation. J Pharmacol Exp Ther. 1990;255(3):1021-1026. 4. Kowala MC, et al. Prostacyclin agonists reduce early atherosclerosis in hyperlipidemic hamsters. Octimibate and BMY 42393 suppress monocyte chemotaxis, macrophage cholesteryl ester accumulation, scavenger receptor activity, and tumor necrosis factor production. Arterioscler Thromb. 1993;13(3):435-44 |