CAS NO: | 141625-93-6 |
生物活性 | Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibitsNa+,K+andCa2+currents. | ||||||||||||||||
体外研究 (In Vitro) | Dronedarone (SR-33589) is a multichannel blocker for atrial fibrillation . 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. Under whole-cell patch clamp, it blocksIKr(IC50=3 μM) andICa-L(IC50=0.18 μM). The effects onICa-Lare use- and frequency-dependent. Dronedarone inhibits current carried by human ether-a-go-go gene (HERG)-expressing oocytes (analagous toIKr) with an IC50of 9 μM[1]. In guinea pig ventricular myocytes, dronedarone exhibits a state dependent inhibition of the fast Na+channel current with an IC50of 0.7±0.1 μM, when the holding potential is –80 mV[2]. | ||||||||||||||||
体内研究 (In Vivo) | Dronedarone (Hydrochloride) reduces significantly the incidence of ventricular fibrillation (VF) from 80 to 30% (p< 0.05) at 3 mg/kg i.v. and eliminated VF and mortality at 10 mg/kg i.v.[3]. Dronedarone inhibited carotid artery thrombus formationin vivo. Thrombin- and collagen-induced platelet aggregation is impaired indronedarone-treated mice (P\0.05), and expression ofplasminogen activator inhibitor-1 (PAI1), an inhibitor of the fibrinolytic system, is reduced in the arterial wall[4]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 593.22 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C31H45ClN2O5S | ||||||||||||||||
CAS 号 | 141625-93-6 | ||||||||||||||||
中文名称 | 决奈达隆盐酸盐;盐酸决奈达隆 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 25 mg/mL(42.14 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液
* 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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