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
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
Zatebradine hydrochloride, ≥98% (HPLC), powder
SMILES string
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
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white
solubility
H2O: >10 mg/mL
originator
Boehringer Ingelheim
storage temp.
2-8°C
Quality Level
Application
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
Biochem/physiol Actions
HCN channel blocker: blocker of neuronal Ih, related cardiac If channels and ATP-sensitive Kir channels.
Zatebradine is a bradycardiac agent.
Features and Benefits
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
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)
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
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)
Cardiomyocyte clusters derived from human embryonic stem cells share similarities with human heart tissue
Asp J, et al.
Journal of Molecular Cell Biology, 2(5), 276-283 (2010)
商品
Cyclic nucleotides like cAMP modulate cell function via PKA activation and ion channels.
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