您好,欢迎来到半岛电竞官方网址 ! [ 登录] [ 免费注册]
半岛电竞官方网址
位置: 首页> 半岛bd体育手机客户端 库> Zatebradine hydrochloride
立即咨询
咨询类型:
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
Zatebradine hydrochloride
本半岛bd体育手机客户端 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 电议
50mg 电议

半岛bd体育手机客户端 介绍
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 SMILES O=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 tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 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.

Baidu
map