ORM-10962_product_DataBase

Bioactivity

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].

Target

NCX.

Invitro

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].

In Vivo

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]. Animal Model:

Name

ORM-10962

CAS

763926-98-3

Formula

C27H29N3O4

Molar Mass

459.54

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

ORM-10962

CAS: 763926-98-3 F: C27H29N3O4 W: 459.54