Zatebradine (hydrochloride)

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). 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. 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.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. CAS Number: 91940-87-3. Synonyms: UL-FS 49. Molecular Formula: C26H36N2O5 . HCl. Formula Weight: 493.0. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 280 nm. SMILES: COC1=CC(CCN(C)CCCN2C(CC(C=C(OC)C(OC)=C3)=C3CC2)=O)=CC=C1OC.Cl. InChi Code: 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.