ORM-10962 (C09-1160-148)

ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC 50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively. ORM-10962 shows antiarrhythmic effectIn VitroORM-10962 (10 nM, 100 nM and 1 μM) decreased the NCX current in dog ventricular myocytes in a concentration-dependent manner with estimated IC 50 values of 55 and 67 nM at -80 and at 20 mV, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoORM-10962 (0.3 mg/kg, IV, once) pre-treatment significantly delays the development and recurrence of ventricular extrasystoles (by about 50%) or ventricular tachycardia (by about 30%) in anesthetized guinea pigs . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male guinea-pigs (250-300 g) Dosage: 0.3 mg/kg Administration: IV, 10 min before starting ouabain infusion Result: Significantly delayed the development of ventricular extrasystoles (from 24±1.7 min in controls to 36.6±2.7 min in the presence of the drug) or ventricular tachycardia (from 31.8±1.8 min in controls to 40.8±2.1 min in the presence of the drug).Form:SolidIC50& Target:NCX. Specification: 0.99 Molecular Formula: C27H29N3O4 Molecular Weight: 459.54 PubChem CID: 69016811 Isomeric SMILES: C1CC2=C(C=CC(=C2)OC3=NC=C(C=C3)NC(=O)CN4CCC(CC4)O)OC1C5=CC=CC=C5