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化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
deionized water: >5 mg/mL
儲存溫度
room temp
SMILES 字串
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 密鑰
NZOSVDHCTCLGEB-UHFFFAOYSA-N
應用
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
生化／生理作用
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.
特點和優勢
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.
訊號詞
Danger
危險聲明
危險分類
Acute Tox. 3 Oral
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Electrophysiological effects of an anti-influenza drug oseltamivir on the guinea-pig atrium: comparison with those of pilsicainide
Takahara A, et al.
Biological & Pharmaceutical Bulletin, 36(10), 1650-1652 (2013)
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)
Masayuki Tasaki et al.
Transplantation, 87(8), 1125-1133 (2009-04-23)
It is generally admitted that ABO(H) blood group antigens are linked to lipids and proteins. Although glycolipids carrying ABO antigens have been well characterized in human kidneys, glycoproteins carrying ABO antigens are largely unknown, and their molecular properties remain to
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
商品
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。
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
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