Eleclazine (hydrochloride)
- Product Name
- Eleclazine (hydrochloride)
- CAS No.
- 1448754-43-5
- Chemical Name
- Eleclazine (hydrochloride)
- Synonyms
- Eleclazine HCl;GS-6615 HYDROCHLORIDE;Eleclazine (hydrochloride);Eleclazine hydrochloride, 10 mM in DMSO;Eleclazine hydrochloride (GS-6615 hydrochloride);4-(Pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one hydrochloride;1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-, hydrochloride (1:1);Inhibitor,Eleclazine,GS-6615,GS6615,porcine,Sodium Channel,KcsA,Eleclazine hydrochloride,Na+ channels,inhibit,Na channels,epinephrine,Potassium Channel,hiPSC,atrial premature beats,GS 6615,cardiac arrhythmias
- CBNumber
- CB53146609
- Molecular Formula
- C21H17ClF3N3O3
- Formula Weight
- 451.83
- MOL File
- 1448754-43-5.mol
Eleclazine (hydrochloride) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);221.32(Max Conc. mM)
- form
- Solid
- color
- White to off-white
- InChI
- 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
- InChIKey
- ZRYHNOXHGYUHFF-UHFFFAOYSA-N
- SMILES
- O=C1N(CCOC2=CC=C(C3C=CC(OC(F)(F)F)=CC=3)C=C12)CC1=NC=CC=N1.Cl
N-Bromosuccinimide Price
- Product number
- CS-5828
- Product name
- Eleclazinehydrochloride
- Purity
- 99.73%
- Packaging
- 1mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-5828
- Product name
- Eleclazinehydrochloride
- Purity
- 99.73%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- orb611433
- Product name
- Eleclazine hydrochloride
- Packaging
- 5mg
- Price
- $569.5
- Updated
- 2021/12/16
- Product number
- CS-5828
- Product name
- Eleclazinehydrochloride
- Purity
- 99.73%
- Packaging
- 10mg
- Price
- $660
- Updated
- 2021/12/16
- Product number
- orb611433
- Product name
- Eleclazine hydrochloride
- Packaging
- 10mg
- Price
- $674.9
- Updated
- 2021/12/16
Eleclazine (hydrochloride) Chemical Properties,Usage,Production
Uses
Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias[1][2][3].
in vivo
Eleclazine (0.3 and 0.9 mg/kg; IV; infused over 15 minutes) reduces the incidence of epinephrine-induced ventricular premature beats and couplets, and shortens ventricular QT and atrial PTa intervals[1].
| Animal Model: | Male Yorkshire pigs (35.20 ± 0.46 kg; injected with epinephrine via a jugular vein)[1] |
| Dosage: | 0.3 and 0.9 mg/kg |
| Administration: | IV; infused over 15 minutes |
| Result: | Reduced the incidence of epinephrine-induced ventricular premature beats and couplets by 51% (from 31.3 ± 1.91 to 15.2 ± 5.08 episodes; P = 0.038) and the incidence of 3- to 7-beat ventricular tachycardia (VT) by 56% (from 10.8 ± 3.45 to 4.7 ± 3.12 episodes; P = 0.004). Shortened ventricular QT and atrial PTa intervals by 7%, and reduced atrial repolarization alternans and heterogeneity without attenuation of the inotropic response to catecholamine. |
References
[1] Bacic D, et al. 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
[2] Rajamani S et al. The novel late Na+ current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations. Br J Pharmacol. 2016 Jul 23. DOI:10.1111/bph.13563
[3] Potet F, Egecioglu DE, Burridge PW, George AL Jr. GS-967 and Eleclazine Block Sodium Channels in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. Mol Pharmacol. 2020 Nov;98(5):540-547. DOI:10.1124/molpharm.120.000048
Eleclazine (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
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