Eleclazine HCl
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MedKoo CAT#: 563723

CAS#: 1448754-43-5 (HCl)

Description: Eleclazine HCl is a novel late Na+ current inhibitor.


Chemical Structure

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Eleclazine HCl
CAS# 1448754-43-5 (HCl)

Theoretical Analysis

MedKoo Cat#: 563723
Name: Eleclazine HCl
CAS#: 1448754-43-5 (HCl)
Chemical Formula: C21H17ClF3N3O3
Exact Mass: 451.0911
Molecular Weight: 451.83
Elemental Analysis: C, 55.82; H, 3.79; Cl, 7.85; F, 12.61; N, 9.30; O, 10.62

Price and Availability

Size Price Availability Quantity
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 750.0 2 Weeks
200.0mg USD 1250.0 2 Weeks
500.0mg USD 2650.0 2 Weeks
1.0g USD 3650.0 2 Weeks
2.0g USD 6450.0 2 Weeks
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Related CAS #: 1443211-72-0 (free base)   1448754-43-5 (HCl)    

Synonym: Eleclazine Hydrochloride; Eleclazine HCl; GS-6615; GS 6615; GS6615;

IUPAC/Chemical Name: 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one hydrochloride

InChi Key: ZRYHNOXHGYUHFF-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H16F3N3O3.ClH/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;1H

SMILES Code: O=C1N(CC2=NC=CC=N2)CCOC3=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=C13.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

Preparing Stock Solutions

The following data is based on the product molecular weight 451.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: El-Bizri N, Xie C, Liu L, Limberis J, Krause M, Hirakawa R, Nguyen S, Tabuena DR, Belardinelli L, Kahlig KM. Eleclazine exhibits enhanced selectivity for long QT syndrome type 3-associated late Na(+) current. Heart Rhythm. 2018 Feb;15(2):277-286. doi: 10.1016/j.hrthm.2017.09.028. Epub 2017 Oct 7. PubMed PMID: 29017927.

2: Wei XH, Yu SD, Ren L, Huang SH, Yang QM, Wang P, Chu YP, Yang W, Ding YS, Huo Y, Wu L. Inhibition of late sodium current suppresses calcium-related ventricular arrhythmias by reducing the phosphorylation of CaMK-II and sodium channel expressions. Sci Rep. 2017 Apr 20;7(1):981. doi: 10.1038/s41598-017-01056-0. PubMed PMID: 28428622; PubMed Central PMCID: PMC5430524.

3: Zhang Y, Wang HM, Wang YZ, Zhang YY, Jin XX, Zhao Y, Wang J, Sun YL, Xue GL, Li PH, Huang QH, Yang BF, Pan ZW. Increment of late sodium currents in the left atrial myocytes and its potential contribution to increased susceptibility of atrial fibrillation in castrated male mice. Heart Rhythm. 2017 Jul;14(7):1073-1080. doi: 10.1016/j.hrthm.2017.01.046. Epub 2017 Feb 6. PubMed PMID: 28185917.

4: Silva AF, Bonatti R, Batatinha JA, Nearing BD, Zeng D, Belardinelli L, Verrier RL. The Selective Late Sodium Current Inhibitor Eleclazine, Unlike Amiodarone, Does Not Alter Defibrillation Threshold or Dominant Frequency of Ventricular Fibrillation. J Cardiovasc Pharmacol. 2017 Mar;69(3):178-182. doi: 10.1097/FJC.0000000000000455. PubMed PMID: 28045761.

5: Bacic D, Carneiro JS, Bento AA, Nearing BD, Rajamani S, Belardinelli L, Verrier RL. 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. Heart Rhythm. 2017 Mar;14(3):448-454. doi: 10.1016/j.hrthm.2016.10.021. Epub 2016 Oct 21. PubMed PMID: 27777148.

6: Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I(Na)i), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties. J Med Chem. 2016 Oct 3. [Epub ahead of print] PubMed PMID: 27690427.

7: Rajamani S, Liu G, El-Bizri N, Guo D, Li C, Chen XL, Kahlig KM, Mollova N, Elzein E, Zablocki J, Belardinelli L. The novel late Na(+) current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations. Br J Pharmacol. 2016 Nov;173(21):3088-3098. doi: 10.1111/bph.13563. Epub 2016 Sep 14. PubMed PMID: 27449698; PubMed Central PMCID: PMC5056228.

8: Justo F, Fuller H, Nearing BD, Rajamani S, Belardinelli L, Verrier RL. 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. Heart Rhythm. 2016 Sep;13(9):1860-7. doi: 10.1016/j.hrthm.2016.06.020. Epub 2016 Jun 16. PubMed PMID: 27317981.

9: Fuller H, Justo F, Nearing BD, Kahlig KM, Rajamani S, Belardinelli L, Verrier RL. 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. Heart Rhythm. 2016 Aug;13(8):1679-86. doi: 10.1016/j.hrthm.2016.04.015. Epub 2016 Apr 21. PubMed PMID: 27108587.