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Zatebradine hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Zatebradine hydrochloride图片
CAS NO:91940-87-3
包装与价格：
包装价格(元)
10mg询价
50mg询价

Zatebradine (UL-FS-49 (free base)) 是一种有效的超极化激活环核苷酸门控 (HCN) 通道抑制剂，IC50 值为 1.96 μM。
Cas No.91940-87-3
别名UL-FS-49; UL-FS-49CL
化学名3-(3-((3,4-dimethoxyphenethyl)(methyl)amino)propyl)-7,8-dimethoxy-4,5-dihydro-1H-benzo[d]azepin-2(3H)-one hydrochloride
Canonical SMILESO=C1N(CCCN(C)CCC(C=C2OC)=CC=C2OC)CCC(C(C1)=C3)=CC(OC)=C3OC.Cl
分子式C26H36N2O5.HCl
分子量493.04
溶解度DMF: 25 mg/mL,DMSO: 20 mg/mL,Ethanol: 1 mg/mL,PBS (pH 7.2): 10 mg/mL
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 μM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 μM, 2.21 μM, 1.90 μM and 1.88 μM, respectively[1].

The use-dependent blockade by Zatebradine of the cardiac pacemaker current from rabbit sino-atrial node cells has an apparent Kd of 480 nM[2].

Zatebradine (0-20 mg/kg; intraperitoneal injection; for 30 minutes; male C57/Bl6-mice) reduces the heart rate dose-dependently from 600 to 200 bpm with ED50 value of 1.8 mg/kg and induces increasing arrhythmia[1].

References:
[1]. Stieber J, et al. Bradycardic and proarrhythmic properties of sinus node inhibitors. Mol Pharmacol. 2006 Apr;69(4):1328-37. Epub 2005 Dec 30.
[2]. Van Bogaert PP, et al. Use-dependent blockade of cardiac pacemaker current (If) by cilobradine and zatebradine. Eur J Pharmacol. 2003 Oct 8;478(2-3):161-71.

 
 
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