[CAS NO. 763926-98-3] ORM-10962
PRODUCTS SPECIFICATIONS [763926-98-3]
DESCRIPTION [763926-98-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 459.54 |
| Molecular Formula | C27H29N3O4 |
| SMILES | O=C(NC1=CC=C(OC2=CC=C3C(CCC(C4=CC=CC=C4)O3)=C2)N=C1)CN5CCC(O)CC5 |
Summary
In Vitro
ORM-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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male guinea-pigs (250-300 g) [1] |
| 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). |
Appearance
Solid
Shipping
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 |
Solvent & Solubility
DMSO : 250 mg/mL ( 544.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1761 mL | 10.8804 mL | 21.7609 mL |
| 5 mM | 0.4352 mL | 2.1761 mL | 4.3522 mL |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1761 mL |
References
- [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.