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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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-5828
Product name
Eleclazinehydrochloride
Purity
99.73%
Packaging
1mg
Price
$180
Updated
2021/12/16
ChemScene
Product number
CS-5828
Product name
Eleclazinehydrochloride
Purity
99.73%
Packaging
5mg
Price
$420
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611433
Product name
Eleclazine hydrochloride
Packaging
5mg
Price
$569.5
Updated
2021/12/16
ChemScene
Product number
CS-5828
Product name
Eleclazinehydrochloride
Purity
99.73%
Packaging
10mg
Price
$660
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611433
Product name
Eleclazine hydrochloride
Packaging
10mg
Price
$674.9
Updated
2021/12/16
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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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Eleclazine (hydrochloride) Suppliers

MQ (shanghai) Pharmaceuticals Co., Ltd.
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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021-65675885 18964387627
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ShangHai Biochempartner Co.,Ltd
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177-54423994 17754423994
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sales@regentsciences.com
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Fan De(Beijing) Biotechnology Co., Ltd.
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15911056312
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Absin Bioscience Inc.
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1448754-43-5, Eleclazine (hydrochloride)Related Search:


  • Eleclazine (hydrochloride)
  • 1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-, hydrochloride (1:1)
  • Eleclazine hydrochloride (GS-6615 hydrochloride)
  • GS-6615 HYDROCHLORIDE
  • Eleclazine HCl
  • 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
  • 4-(Pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one hydrochloride
  • Eleclazine hydrochloride, 10 mM in DMSO
  • 1448754-43-5