Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class IIIantiarrhythmic agentfor the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multipleion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4^[1].

In patch clamp experiments using human atrial myocytes, Dronedarone produces potent blockade of peak sodium current, resulting in a 97% block at 3 μM^[1].
In guinea pig ventricular myocytes, Dronedarone inhibits the rapidly activating delayed-rectifier potassium current (IC₅₀<3 μm), the slowly activating delayed-rectifier potassium current (ic₅₀=10 μM), the inward rectifier potassium current (IC₅₀>30 μM), and L-type calcium current (IC₅₀=0.18 μM)^[1].
Dronedarone exhibits strong inhibitory effects on the acetylcholine-activated potassium current (I_K-Ach) in rabbit inoatrial nodal cells (IC₅₀=63 nM) and guinea pig atrial cells (IC₅₀=10 nM). Blockade of I_K-Achby dronedarone is 100 times more potent than that of amiodarone^[1].
Dronedarone exerts its antiadrenergic effects by noncompetitive binding to β-adrenergic receptors (IC₅₀=1.8 μM) and inhibition of agonist-induced increases in adenylate cyclase activity^[1].
Dronedarone (0.01-1 μM) induces a concentration-dependent reduction of coronary perfusion pressure in isolated guinea pig hearts, effects that are independent of the nitric oxide synthase pathway and possibly related to its calcium current blockade^[1].

Dronedarone (intraperitoneal injection; 25-100 mg/kg) exhibits anticonvulsant effects in a dose-dependent manner and increases the threshold for electroconvulsions in mice^[2].

556.76

Solid

C₃₁H₄₄N₂O₅S

141626-36-0

决奈达隆；决奈达龙

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL(89.81 mM;Need ultrasonic)

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• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.49 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.49 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.5 mg/mL (4.49 mM); Suspended solution

  此方案可获得 ≥ 2.5 mg/mL (4.49 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (4.49 mM); Suspended solution

  此方案可获得 ≥ 2.5 mg/mL (4.49 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。