Dronedarone HCl
(Synonyms: 盐酸决奈达隆) 目录号 : GC12234An antiarrhythmic agent
Cas No.:141625-93-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
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Animal experiment: | Rats: Rats are anesthetized, artificially ventilated, and the thorax opened by a left thoracotomy. Ischemia is induced by left coronary artery ligation, and reperfusion is achieved (after a 5-min period of ischemia) in a separate group of rats by removing the ligature. Agents are given intravenously 5 min before occlusion or orally 4 h before study[3]. Mice: Twelve-week-old C57Bl/6 mice are divided into two groups: dronedarone (200 mg/kg body weight with a once daily oral gavage for 14 days) or control (1.4 % methylcellulose). Twenty-four hours after the last application, mice are anesthetized by intraperitoneal injection of 87 mg/kg sodium pentobarbital. Rose bengal is diluted to 12 mg/mL in phosphate-buffered saline and then injected into the tail vein at a concentration of 63 mg/kg[4]. |
References: [1]. Bogdan R, et al. Effect of dronedarone on Na+, Ca2+ and HCN channels. Naunyn Schmiedebergs Arch Pharmacol. 2011 Apr;383(4):347-56. |
Dronedarone HCL is an amiodarone analogue which has been shown an effective and promising treatment for Atrial fibrillation (AF) [1].
In vitro, dronedarone has been demonstrated to inhibit muscarinic acetylcholine receptor-operated K+ current IK(ACh) induced by carbachol or GTP-gamma-S with IC50 values of 10nm and <100nm, respectively, in cells isolated from guinea pig atria. Notably, dronedarone was 100-fold potent and selective over amiodarone in inhibiting IK(ACh) [1].
In vivo, dronedarone has shown to block arterial thrombus formation, decrease platelet aggregation and reduce plasminogen activator inhibitor-1 (PAI1) expression in C57Bl/6 mice [2].
References:
[1] Guillemare E1, Marion A, Nisato D, Gautier P. Inhibitory effects of dronedarone on muscarinic K+ current in guinea pig atrial cells. J Cardiovasc Pharmacol. 2000 Dec;36(6):802-5.
[2] Breitenstein A1, Sluka SH, Akhmedov A, Stivala S, Steffel J, Camici GG, Riem HH, Beer HJ, Studt JD, Duru F, Luscher TF, Tanner FC. Dronedarone reduces arterial thrombus formation. Basic Res Cardiol. 2012 Nov;107(6):302.
Cas No. | 141625-93-6 | SDF | |
别名 | 盐酸决奈达隆 | ||
化学名 | N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-1-benzofuran-5-yl]methanesulfonamide;hydrochloride | ||
Canonical SMILES | CCCCC1=C(C2=C(O1)C=CC(=C2)NS(=O)(=O)C)C(=O)C3=CC=C(C=C3)OCCCN(CCCC)CCCC.Cl | ||
分子式 | C31H45ClN2O5S | 分子量 | 593.22 |
溶解度 | ≥ 28.25mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.6857 mL | 8.4286 mL | 16.8572 mL |
5 mM | 0.3371 mL | 1.6857 mL | 3.3714 mL |
10 mM | 0.1686 mL | 0.8429 mL | 1.6857 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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