Dronedarone-Hydrochloride - Potassium Channel 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDronedarone HydrochlorideCat. No.: HY-75839CAS No.: 141625-93-6分式: CHClNOS分量: 593.22作靶點: Potassium Channel; Autophagy作通路: Membrane Transporter/Ion Channel; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C

2、1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (84.29 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6857 mL 8.4286 mL 16.8572 mL5 mM 0.3371 mL 1.6857 mL 3.3714 mL10 mM 0.1686 mL 0.8429 mL 1.6857 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜?/p>

3、解案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (5.06 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (5.06 mM); Clear solution3.

4、請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 3 mg/mL (5.06 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Dronedarone Hydrochloride種碘化胺碘酮衍物, 可抑制Na+, K+ and Ca2+的電流。體外研究 Dronedarone (SR-33589) is a multichannel blocker for atrial fibrillation . It is a poten

5、t inhibitor of theacetylcholine-activated K+ current from atrial and sinoatrial nodal tissue, and inhibits the rapid delayedrectifier more potently than slow and inward rectifier K+ currents and inhibits L-type calcium current. Underwhole-cell patch clamp, it blocks IKr (IC50=3 M) and ICa-L (IC50=0.

6、18 M). The effects on ICa-L are use-and frequency-dependent. Dronedarone inhibits current carried by human ether-a-go-go gene (HERG)-expressing oocytes (analagous to IKr) with an IC50 of 9 M 1. In guinea pig ventricular myocytes,dronedarone exhibits a state dependent inhibition of the fast Na+ chann

7、el current with an IC50 of 0.70.1 M,when the holding potential is 80 mV 2.體內(nèi)研究 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 carotidarte

8、ry thrombus formation in vivo. Thrombin- and collagen-induced platelet aggregation is impairedindronedarone-treated mice (P0.05), and expression ofplasminogen activator inhibitor-1 (PAI1), an inhibitorof the fibrinolytic system, is reduced in the arterial wall 4.PROTOCOLAnimal Rats: Rats are anesthe

9、tized, artificially ventilated, and the thorax opened by a left thoracotomy. Ischemia isAdministration 34 induced by left coronary artery ligation, and reperfusion is achieved (after a 5-min period of ischemia) in aseparate group of rats by removing the ligature. Agents are given intravenously 5 min

10、 before occlusion ororally 4 h before study 3.Mice: Twelve-week-old C57Bl/6 mice are divided into two groups: dronedarone (200 mg/kg body weight witha once daily oral gavage for 14 days) or control (1.4 % methylcellulose). Twenty-four hours after the lastapplication, mice are anesthetized by intrape

11、ritoneal injection of 87 mg/kg sodium pentobarbital. Rose bengalis diluted to 12 mg/mL in phosphate-buffered saline and then injected into the tail vein at a concentration of63 mg/kg 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Bogdan

12、R, et al. Effect of?dronedarone?on Na+, Ca2+ and HCN channels. Naunyn Schmiedebergs Arch Pharmacol.?2011Apr;383(4):347-56.?2. Doggrell SA, et al. Dronedarone: an amiodarone analogue. Expert Opin Investig Drugs. 2004 Apr;13(4):415-26.3. Manning AS, et al. SR 33589, a new amiodarone-like agent: effect on ischemia- and reperfusion-induced arrhythmias in anesthetizedrats. J Cardiovasc Pharmacol. 1995 Sep;26(3):453-61.4. Breitenstein A, et al. Dronedarone reduces arterial thrombus formation. Basic Res Cardiol. 2012 Nov;107(6):302.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHe