Eleclazine hydrochloride (GS 6615 hydrochloride) (Synonyms: GS 6615 hydrochloride) |
Catalog No.GC30063
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Eleclazine hydrochloride (GS 6615 hydrochloride) est un nouveau médicament super sélectif qui inhibe le courant sodique tardif cardiaque, sa valeur d'IC50 est <1μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1448754-43-5
Sample solution is provided at 25 µL, 10mM.
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Eleclazine hydrochloride (GS 6615 hydrochloride) est un nouveau médicament super sélectif qui inhibe le courant sodique tardif cardiaque, sa valeur d'IC50 est <1μM[1]. Eleclazine hydrochloride (GS 6615 hydrochloride) stabilise la possibilité membranaire cardiaque, arrête les arythmies par voie de réduire la surcharge intracellulaire en sodium et calcium. On l'utilise beaucoup pour traiter, étudier les troubles du rythme comme le syndrome de QT long et la tachycardie ventriculaire[2,3,4].
Le pré-traitement in vitro avec Eleclazine hydrochloride (GS 6615 hydrochloride) (1μM) aux coeurs de lapin isolés pendant 20 minutes a significativement accéléré la disparition du calcium intracellulaire, empêché l'apparition d'alternances spatiales discordantes (ASD) dans les conditions normothermiques[5]. Le traitement avec Eleclazine hydrochloride (GS 6615 hydrochloride) (10μM) aux cardiomyocytes auriculaires de lapin isolés pendant 5 minutes a réduit de 41% la densité du courant sodique tardif provoqué par l'isoprotérénol (ISO, 15nM) (p < 0.05)[6].
Les porcs Yorkshire pré-traités in vivo avec Eleclazine hydrochloride (GS 6615 hydrochloride) (0.9mg/kg; perfusion intraveineuse pendant 15 minutes) ont présenté leur incidence de contractions prématurées auriculaires (CPA) de 1 à 2 battements diminuer de 83%, et celle de CPA de 3 battements ou plus de 75%, 120 minutes après l'administration, quand on leur a injecté de l'épinéphrine (2,0 µg/kg en bolus intraveineux pendant 1 minute)[7].
References:
[1] BACIC D, CARNEIRO J S, BENTO A A, et al. Eleclazine hydrochloride (GS 6615 hydrochloride), 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[J]. Heart Rhythm, 2017, 14(3): 448-454.
[2] RAJAMANI S, LIU G, EL-BIZRI N, et al. The novel late Na+ current inhibitor, GS-6615 (Eleclazine hydrochloride (GS 6615 hydrochloride)) and its anti-arrhythmic effects in rabbit isolated heart preparations[J]. British Journal of Pharmacology, 2016, 173(21): 3088-3098.
[3] POTET F, EGECIOGLU D E, BURRIDGE P W, et al. GS-967 and Eleclazine hydrochloride (GS 6615 hydrochloride) block sodium channels in human induced pluripotent stem cell-derived cardiomyocytes[J]. Molecular Pharmacology, 2020, 98(5): 540-547.
[4] ZHANG Y, WANG H M, WANG Y Z, et al. Increment of late sodium currents in the left atrial myocytes and its potential contribution to increased susceptibility of atrial fibrillation in castrated male mice[J]. Heart Rhythm, 2017, 14(7): 1073-1080.
[5] LEE H L, CHANG P C, WO H T, et al. Eleclazine hydrochloride (GS 6615 hydrochloride) suppresses ventricular fibrillation in failing rabbit hearts with ischemia-reperfusion injury undergoing therapeutic hypothermia[J]. Pharmacology, 2025, 110(3): 151-164.
[6] LIU X, REN L, YU S, et al. Late sodium current in synergism with Ca2+/calmodulin-dependent protein kinase II contributes to β-adrenergic activation-induced atrial fibrillation[J]. Philosophical Transactions of the Royal Society B: Biological Sciences, 2023, 378(1879).
[7] FULLER H, JUSTO F, NEARING B D, et al. Eleclazine hydrochloride (GS 6615 hydrochloride), 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[J]. Heart Rhythm, 2016, 13(8): 1679-1686.
| Expériences cellulaires [1]: | |
Lignées cellulaires | Atrial myocytes |
Méthode de préparation | On a prélevé les cardiomyocytes auriculaires sur les coeurs de lapin, puis on les a traités 5 minutes avec 15nM d'ISO, soit sans Eleclazine hydrochloride (GS 6615 hydrochloride), soit avec 10µM de Eleclazine hydrochloride (GS 6615 hydrochloride). On a ensuite mesuré le courant sodique tardif (late INa) grâce à la technique du patch-clamp en configuration "cellule entière". |
Conditions de réaction | 10μM; 5min |
Domaines d'application | Le traitement avec Eleclazine hydrochloride (GS 6615 hydrochloride) a réduit de 41% la densité du courant sodique tardif provoqué par ISO (p < 0.05). |
| Expériences animales [2]: | |
Modèles animaux | Porcs Yorkshire |
Méthode de préparation | Les porcs Yorkshire ont reçu une perfusion intraveineuse de 0.9mg/kg d' Eleclazine hydrochloride (GS 6615 hydrochloride) pendant 15 minutes. On a ensuite analysé l'incidence des contractions prématurées auriculaires (APBs) induites par l'épinéphrine à plusieurs moments (60, 90, 120, 150min). |
Forme de dosage | 0.9mg/kg; 120min; i.v. |
Domaines d'application | Le traitement avec Eleclazine hydrochloride (GS 6615 hydrochloride) a réduit de 83% APBs de 1 à 2 battements et de 75% APBs de 3 battements ou plus, tous provoqués par l'épinéphrine. |
References: | |
| Cas No. | 1448754-43-5 | SDF | |
| Synonymes | GS 6615 hydrochloride | ||
| Canonical SMILES | O=C1N(CC2=NC=CC=N2)CCOC3=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=C13.[H]Cl | ||
| Formula | C21H17ClF3N3O3 | M.Wt | 451.83 |
| Solubility | DMSO : ≥ 100 mg/mL (221.32 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2132 mL | 11.0661 mL | 22.1322 mL |
| 5 mM | 442.6 μL | 2.2132 mL | 4.4264 mL |
| 10 mM | 221.3 μL | 1.1066 mL | 2.2132 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)