Blocks If currents through HCN channels in sinoatrial node cells (IC50s = 1.83

Zatebradine (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
91940-87-3
Storage:
-20
UN-No:
Non-Hazardous - /

Zatebradine is a bradycardic compound that blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells (IC50s = 1.83, 2.21, 1.9, and 1.88 µM, respectively for HCN1-4 in vitro).{30118,25789} Additionally, it can block voltage-gated outward K+ (IK) currents and related neuronal hyperpolarization-activated inward current (Ih) channels, but exhibits little or no activity for L-type Ca2+ (ICa) currents.{30117,28049} When assessed through telemetric ECG recording in mice, zatebradine reduced heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induced increasing arrhythmia at concentrations >10 mg/kg.{30118}  

 

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Description

Blocks If currents through HCN channels in sinoatrial node cells (IC50s = 1.83, 2.21, 1.9, and 1.88 µM, respectively for HCN1-4 in vitro); reduces heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induces increasing arrhythmia at concentrations >10 mg/kg when assessed through telemetric ECG recording in mice

Formal name: 3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one, monohydrochloride

Synonyms:  UL-FS 49

Molecular weight: 493

CAS: 91940-87-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Neuroscience

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