|N-(2-丁基-3-(4-(3-(二丁基氨基)丙氧基)苯甲酰基)苯并呋喃-5-基)甲磺酰胺盐酸盐|CsnPharm

CAS No.: 141625-93-6

盐酸决奈达隆 Catalog No. CSN10870

Synonyms: SR33589;Dronedarone (hydrochloride);4CH-007232

Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Dronedarone hHydrochloride, is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents. It is a potent inhibitor of the acetylcholine-activated K+ current from atrial and sinoatrial nodal tissue, and inhibits the rapid delayed rectifier more potently than slow and inward rectifier K+ currents and inhibits L-type calcium current. Dronedarone is an antagonist at alpha- and beta-adrenoceptors and unlike amiodarone, has little effect at thyroid receptors^[3]. Intravenous administration of dronedarone hydrochloride in doses of 0.3 and 3 mg/kg over 30s attained the peak plasma concentrations of 61 and 1248 ng/mL, respectively, reflecting sub- to supra-therapeutic ones. The low dose decreased the left ventricular contraction and mean blood pressure, which were enhanced at the high dose. The high dose also decreased the heart rate and cardiac output, but increased the total peripheral resistance and left ventricular end-diastolic pressure, showing its potent cardiodepressive profile. Dronedarone significantly prolonged the T(peak)-T(end) in a dose-related manner with a tendency to prolong the terminal repolarization period and J-Tpeakc, indicating considerable risk to induce torsade de pointes^[4]. Improved oral bioavailability of dronedarone could be provided by an optimized proliposomal formulation with enhanced solubility, permeability, and oral absorption^[5]. In guinea pig ventricular myocytes, dronedarone exhibited a state-dependent inhibition of the fast Na(+) channel current with an IC(50) of 0.7 ± 0.1 μM, when the holding potential (V (hold)) was -80 mV. The maximal block at the highest concentration used was 77 ± 8%. In contrast, when V (hold) was -100 mV, inhibition with 10 μM dronedarone was only 9 ± 3% (n = 7). Dronedarone blocked Ca(2+) currents elicited by rectangular pulses at V (hold) = -40 mV with an IC(50) value of 0.4 ± 0.1 μM (maximal block by 10 μM dronedarone, 80 ± 6%), whereas at V (hold) = -80 mV, 10 μM dronedarone blocked only 20 ± 6% (n = 4) of the current. Inhibition of fast Na+ and Ca2+ channels by dronedarone depends on the cell's resting membrane potential (state-dependent block) favouring an atrialselective mode of action. Besides fast Na+ and Ca2+ channels, dronedarone also inhibits HCN4 currents. This might contribute to the clinically observed reduction in heart rate seen in patients in sinus rhythm after dronedarone treatment^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

141625-93-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H45ClN2O5S

运输

蓝冰

分子量

593.22

别名

SR33589;Dronedarone (hydrochloride);4CH-007232;D4689;W3083;D03914;S-7529;MCULE-2160502046;RL01735;RTC-070901;AK-72887;BC201083;BR-72887;KB-76727;AB2000517;ST2413542;Dronedarone HCl;UNII-FA36DV299Q;盐酸决奈达隆

溶解度

DMSO	80.0 mg/mL (134.9 mM)
Water	Insoluble
Ethanol	39.0 mg/mL (65.7 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

盐酸决奈达隆 Catalog No. CSN10870

靶点选择性

请登录您的专属账户

确认信息