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Merck
CN

Z0127

Zatebradine hydrochloride

≥98% (HPLC), HCN channel blocker, powder

别名:

7,8-Dimethoxy-3-[3-[-N-[2-(3,4 dimethoxyphenyl)ethyl]-N-methylamino]propyl]-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one hydrochloride, UL-FS49

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关于此项目

经验公式(希尔记法):
C26H37ClN2O5
化学文摘社编号:
分子量:
493.04
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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产品名称

Zatebradine hydrochloride, ≥98% (HPLC), powder

质量水平

方案

≥98% (HPLC)

表单

powder

储存条件

desiccated

颜色

white

溶解性

H2O: >10 mg/mL

创始人

Boehringer Ingelheim

储存温度

2-8°C

SMILES字符串

Cl[H].COc1ccc(CCN(C)CCCN2CCc3cc(OC)c(OC)cc3CC2=O)cc1OC

InChI

1S/C26H36N2O5.ClH/c1-27(13-9-19-7-8-22(30-2)23(15-19)31-3)11-6-12-28-14-10-20-16-24(32-4)25(33-5)17-21(20)18-26(28)29;/h7-8,15-17H,6,9-14,18H2,1-5H3;1H

InChI key

ZRNKXJHEQKMWCH-UHFFFAOYSA-N

应用

Zatebradine hydrochloride has been used:
  • as an If blocker to study its effects on cardiomyocyte clusters (CMCs)
  • as a hyperpolarization-activated and cyclic nucleotide-gated (HCN) channel inhibitor to study its effects on viability of degenerating rod or cone photoreceptors in mice
  • as a bradycardiac agent to study its effects on tachycardia and elevated temperature in fish

生化/生理作用

HCN channel blocker: blocker of neuronal Ih, related cardiac If channels and ATP-sensitive Kir channels.
Zatebradine is a bradycardiac agent.

特点和优势

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Boehringer Ingelheim. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)

法规信息

新产品
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分析证书(COA)

Lot/Batch Number

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访问文档库

Hiroko Izumi-Nakaseko et al.
Journal of pharmacological sciences, 135(1), 44-50 (2017-09-21)
Human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) have been used in many studies to assess proarrhythmic risks of chemical compounds. In those studies, field potential durations (FPD) of hiPSC-CMs have been corrected by clinically used Fridericia's and/or Bazett's formulae, however
Christopher M Wilson et al.
Comparative biochemistry and physiology. Part A, Molecular & integrative physiology, 164(1), 258-263 (2012-09-27)
Pharmacological ion-channel blockers were used to investigate the spontaneous heart rates in Pacific hagfish, Eptatretus stoutii. Zatebradine, a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker, vastly reduced atrial and ventricular contraction rates in a similar concentration-dependent manner, indicating a major role
Effects of zatebradine and propranolol on canine ischemia and reperfusion-induced arrhythmias
Naito H, et al.
European Journal of Pharmacology, 388(2), 171-176 (2000)
Loss of HCN1 enhances disease progression in mouse models of CNG channel-linked retinitis pigmentosa and achromatopsia
Schon C, et al.
Human Molecular Genetics, 25(6), 1165-1175 (2016)
William Joyce et al.
Journal of comparative physiology. B, Biochemical, systemic, and environmental physiology, 188(3), 481-490 (2017-10-27)
The amount of blood pumped by the heart (cardiac output) must be matched to the amount of blood returning to the heart (venous return), but the factors determining cardiac filling are sparsely understood in ectothermic vertebrates. Stroke volume is affected

商品

Cyclic nucleotides like cAMP modulate cell function via PKA activation and ion channels.

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