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关于此项目
经验公式(希尔记法):
C17H24N2O · xHCl
化学文摘社编号:
分子量:
272.39 (free base basis)
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
deionized water: >5 mg/mL
storage temp.
room temp
SMILES string
Cl.Cc1cccc(C)c1NC(=O)CC23CCCN2CCC3
InChI
1S/C17H24N2O.ClH/c1-13-6-3-7-14(2)16(13)18-15(20)12-17-8-4-10-19(17)11-5-9-17;/h3,6-7H,4-5,8-12H2,1-2H3,(H,18,20);1H
InChI key
NZOSVDHCTCLGEB-UHFFFAOYSA-N
Application
Pilsicainide hydrochloride has been used as a sodium channel blocker:
- to study its effects on electrophysiological parameters in guinea pig pulmonary vein preparation
- to study its effects on Ca2+ release and arrhythmic events in Andersen-Tawil syndrome induced pluripotent stem cells (ATS-iPSC)-derived cardiomyocytes
- to study its electrophysiological effects on the guinea pig atrium
Biochem/physiol Actions
Pilsicainide hydrochloride is a pure sodium channel blocker and an open channel blocker of Na+1 channels.
Pilsicainide hydrochloride is a pure sodium channel blocker and an open channel blocker of Na+1 channels. Pilsicainide was defined as a pure sodium channel blocker. The compound is classified as a class Ic antiarrhythmic drug, and was originally developed in Japan. Similar to Lidocaine, Pilsicainide binds to open channels, but slowly. Pilsicainide is capable of selectively blocking the late currents in the mutant Na(+) channels that show dominant abnormal burst openings such as in δKPQ mutants. The compound is used to induce Brugada syndrome (BS) in animal models.
Features and Benefits
This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
商品
Voltage-gated sodium channels are present in most excitable cell membranes and play an important role in generating action potentials.
Discover Bioactive Small Molecules for ADME/Tox
电压门控钠通道存在于大多数可兴奋细胞膜中,在产生动作电位方面起着重要作用。
Flecainide ameliorates arrhythmogenicity through NCX flux in Andersen-Tawil syndrome-iPS cell-derived cardiomyocytes
Kuroda Y, et al.
Biochemistry and Biophysics Reports, 9(4), 245-256 (2017)
Electrophysiological effects of the class Ic antiarrhythmic drug pilsicainide on the guinea-pig pulmonary vein myocardium
Takahara A, et al.
Journal of Pharmacological Sciences, 118(4), 506-511 (2012)
Suchitra Matsukura et al.
Journal of pharmacological sciences, 133(2), 103-109 (2017-03-02)
We pharmacologically characterized microminipigs as an in vivo experimental model by assessing cardiovascular effects of pilsicainide, verapamil and E-4031, which can preferentially inhibit cardiac Na
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| P0026-10MG | 04061832575162 |
| P0026-50MG | 04061832575179 |
