For research use only. Not for therapeutic Use.
Eleclazine（Cat No.:I006637）, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for the treatment of coronary vasodilators, antiarrhythmics, and vasodilators. Eleclazin showed a shortening of the QTc interval (the time interval between the start of the Q-wave and the end of the T-wave in the heart’s electrical cycle) in patients with long QT-3 (LQT3) syndrome. LQT3 is a genetic disorder that prolongs the heart’s QTc interval and can cause life-threatening cardiac arrhythmias (abnormal heartbeats).
| Catalog Number | I006637 |
| CAS Number | 1443211-72-0 |
| Synonyms | GS-6615; GS 6615; GS6615; Eleclazine.;4-[(pyrimidin-2-yl)methyl]-7-[4-(trifluoromethoxy)phenyl]- 3,4-dihydro-1,4-benzoxazepin-5(2H)-one |
| Molecular Formula | C21H16F3N3O3 |
| Purity | ≥95% |
| Target | sodium current inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 2-8°C |
| IUPAC Name | 4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazepin-5-one |
| InChI | InChI=1S/C21H16F3N3O3/c22-21(23,24)30-16-5-2-14(3-6-16)15-4-7-18-17(12-15)20(28)27(10-11-29-18)13-19-25-8-1-9-26-19/h1-9,12H,10-11,13H2 |
| InChIKey | YNUAEEJQYHYLMS-UHFFFAOYSA-N |
| SMILES | C1COC2=C(C=C(C=C2)C3=CC=C(C=C3)OC(F)(F)F)C(=O)N1CC4=NC=CC=N4 |
| Reference | </br>1:The Selective Late Sodium Current Inhibitor Eleclazine, Unlike Amiodarone, Does Not Alter Defibrillation Threshold or Dominant Frequency of Ventricular Fibrillation. Silva AF, Bonatti R, Batatinha JA, Nearing BD, Zeng D, Belardinelli L, Verrier RL.J Cardiovasc Pharmacol. 2017 Mar;69(3):178-182. doi: 10.1097/FJC.0000000000000455. PMID: 28045761 </br>2:Eleclazine, an inhibitor of the cardiac late sodium current, is superior to flecainide in suppressing catecholamine-induced ventricular tachycardia and T-wave alternans in an intact porcine model. Bacic D, Carneiro JS, Bento AA, Nearing BD, Rajamani S, Belardinelli L, Verrier RL.Heart Rhythm. 2017 Mar;14(3):448-454. doi: 10.1016/j.hrthm.2016.10.021. Epub 2016 Oct 21. PMID: 27777148 </br>3:The novel late Na<sup>+</sup> current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations. Rajamani S, Liu G, El-Bizri N, Guo D, Li C, Chen XL, Kahlig KM, Mollova N, Elzein E, Zablocki J, Belardinelli L.Br J Pharmacol. 2016 Nov;173(21):3088-3098. doi: 10.1111/bph.13563. Epub 2016 Sep 14. PMID: 27449698 </br>4:Inhibition of the cardiac late sodium current with eleclazine protects against ischemia-induced vulnerability to atrial fibrillation and reduces atrial and ventricular repolarization abnormalities in the absence and presence of concurrent adrenergic stimulation. Justo F, Fuller H, Nearing BD, Rajamani S, Belardinelli L, Verrier RL.Heart Rhythm. 2016 Sep;13(9):1860-7. doi: 10.1016/j.hrthm.2016.06.020. Epub 2016 Jun 16. PMID: 27317981 </br>5:Eleclazine, a new selective cardiac late sodium current inhibitor, confers concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in an intact porcine model. Fuller H, Justo F, Nearing BD, Kahlig KM, Rajamani S, Belardinelli L, Verrier RL.Heart Rhythm. 2016 Aug;13(8):1679-86. doi: 10.1016/j.hrthm.2016.04.015. Epub 2016 Apr 21. PMID: 27108587 |
