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Merck
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Key Documents

SML2938

Sigma-Aldrich

Vernakalant hydrochloride

≥98% (HPLC)

Sinónimos:

(3R)-1-((1R,2R)-2-(2-(3,4-Dimethoxyphenyl)ethoxy)cyclohexyl)pyrrolidin-3-ol hydrochloride, (3R)-1-[(1R,2R)-2-[2-(3,4-Dimethoxyphenyl)ethoxy]cyclohexyl]-3-pyrrolidinol hydrochloride, RSD 1235, RSD-1235, RSD1235

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About This Item

Fórmula empírica (notación de Hill):
C20H31NO4 · HCl
Número de CAS:
Peso molecular:
385.93
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

Análisis

≥98% (HPLC)

formulario

powder

condiciones de almacenamiento

desiccated

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear

temp. de almacenamiento

−20°C

InChI

1S/C20H31NO4.ClH/c1-23-19-8-7-15(13-20(19)24-2)10-12-25-18-6-4-3-5-17(18)21-11-9-16(22)14-21;/h7-8,13,16-18,22H,3-6,9-12,14H2,1-2H3;1H/t16-,17-,18-;/m1./s1

Clave InChI

JMHYCBFEEFHTMK-IIUXMCBISA-N

Acciones bioquímicas o fisiológicas

Vernakalant is a multiple ion channel blocker that exerts in vivo anti-fibrillatory (anti-arrhythmic) efficacy (ED50 = 1.5 μmol/kg/min iv. against ischemia-induced arrhythmias in rats) via atrial-selective Kv1.5 blockage (hKv1.5/rKv4.2/rKv4.3 IC50 = 13/38/30 μM at 1Hz & -80 to 60 mV in 200 (Kv1.5) or 400 (Kv4) msec) as well as potential- and rate-dependent Nav1.5 blockade (inward Na current INa IC50 = 9 μM/20 Hz & -80 mV, 31 μM/1Hz & -60 mV, 107 μM/1Hz & -120 mV using HEK hNav1.5 cells).

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


Certificados de análisis (COA)

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Rong Chen et al.
Biochemistry, 57(18), 2704-2710 (2018-04-14)
Molecular dynamics simulations are employed to determine the inhibitory mechanisms of three drugs, 5-(4-phenoxybutoxy)psoralen (PAP-1), vernakalant, and flecainide, on the voltage-gated K+ channel Kv1.5, a target for the treatment of cardiac arrhythmia. At neutral pH, PAP-1 is neutral, whereas the
Jonas Goldin Diness et al.
Circulation. Arrhythmia and electrophysiology, 10(10) (2017-10-12)
Evidence has emerged that small-conductance Ca2+-activated K+ (SK) channels constitute a new target for treatment of atrial fibrillation (AF). SK channels are predominantly expressed in the atria as compared with the ventricles. Various marketed antiarrhythmic drugs are limited by ventricular
Gerrit Frommeyer et al.
Europace : European pacing, arrhythmias, and cardiac electrophysiology : journal of the working groups on cardiac pacing, arrhythmias, and cardiac cellular electrophysiology of the European Society of Cardiology, 19(5), 866-873 (2016-10-06)
The antiarrhythmic drug vernakalant exerts antiarrhythmic effects in atrial fibrillation. Recent experimental data suggest interactions with the late sodium current and antiarrhythmic effects in ventricular arrhythmias. We aimed at investigating whether treatment with vernakalant reduces polymorphic ventricular tachycardia (VT) in
Toshiki Chiba et al.
Journal of pharmacological sciences, 130(3), 170-176 (2016-04-02)
Electrical remodeling plays a pivotal role in maintaining the reentry during atrial fibrillation. In this study, we assessed influence of electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. We used an atrial electrical remodeling model of the
Gerrit Frommeyer et al.
Journal of cardiovascular medicine (Hagerstown, Md.), 18(9), 663-668 (2017-07-12)
Current guidelines recommend vernakalant for pharmacologic cardioversion of recent-onset atrial fibrillation. However, this drug is not established as chronic therapy. In total, 15 rabbit hearts were Langendorff-perfused. A burst pacing protocol-induced atrial fibrillation in 7 of 15 hearts at baseline

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