For research use only. Not for therapeutic Use.
ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively. ORM-10962 shows antiarrhythmic effect[1][2][3].
ORM-10962 (10 nM, 100 nM and 1 μM) decreased the NCX current in dog ventricular myocytes in a concentration-dependent manner with estimated IC50 values of 55 and 67 nM at -80 and at 20 mV, respectively[1].
ORM-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[1].
| Catalog Number | I019019 |
| CAS Number | 763926-98-3 |
| Synonyms | 2-(4-hydroxypiperidin-1-yl)-N-[6-[(2-phenyl-3,4-dihydro-2H-chromen-6-yl)oxy]pyridin-3-yl]acetamide |
| Molecular Formula | C27H29N3O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H29N3O4/c31-22-12-14-30(15-13-22)18-26(32)29-21-7-11-27(28-17-21)33-23-8-10-25-20(16-23)6-9-24(34-25)19-4-2-1-3-5-19/h1-5,7-8,10-11,16-17,22,24,31H,6,9,12-15,18H2,(H,29,32) |
| InChIKey | UPGUBLDTYLMRHO-UHFFFAOYSA-N |
| SMILES | C1CC2=C(C=CC(=C2)OC3=NC=C(C=C3)NC(=O)CN4CCC(CC4)O)OC1C5=CC=CC=C5 |
| Reference | [1]. Kohajda Z, et al. The Effect of a Novel Highly Selective Inhibitor of the Sodium/Calcium Exchanger (NCX) on Cardiac Arrhythmias in In Vitro and In Vivo Experiments. PLoS One. 2016 Nov 10;11(11):e0166041. [2]. Oravecz K, et al. Inotropic effect of NCX inhibition depends on the relative activity of the reverse NCX assessed by a novel inhibitor ORM-10962 on canine ventricular myocytes. Eur J Pharmacol. 2018 Jan 5;818:278-286. [3]. Kohajda Z, et al. Novel Na+/Ca2+ Exchanger Inhibitor ORM-10962 Supports Coupled Function of Funny-Current and Na+/Ca2+ Exchanger in Pacemaking of Rabbit Sinus Node Tissue. Front Pharmacol. 2020 Jan 29;10:1632. |
