Dronedarone是胺碘酮的衍生物,是一种用于研究心房颤动(AF)的 III 类抗心律失常试剂。它是多种离子电流(包括钾电流、钠电流和 L 型钙电流)的有效阻滞剂,并通过非竞争性结合肾上腺素能受体发挥抗肾上腺素能作用。此外,Dronedarone 是 CYP3A4 的底物和中度抑制剂,广泛用于心律失常机制和药理研究。
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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK2, IC50: 711 nM ULK1, IC50: 108 nM |
95% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
99% | |||||||||||||||||
Lys05 | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | AChE ↓ ↑ | AChR ↓ ↑ | mAChR ↓ ↑ | nAChR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Donepezil |
+++
bAChE, IC50: 8.12 nM hAChE, IC50: 11.6 nM |
98% | |||||||||||||||||
Loganin |
++
AChE, IC50: 3.95 μM |
99%+ | |||||||||||||||||
topride HCl |
++
AChE, IC50: 2.04 μM |
98% | |||||||||||||||||
Dehydroevodiamine HCl | ✔ | 99%+ | |||||||||||||||||
Jatrorrhizine |
++
AChE, IC50: 872 nM |
99%+ | |||||||||||||||||
Palmatine |
++
AChE, IC50: 0.51 μM |
98% | |||||||||||||||||
(-)-Huperzine A |
++++
AChE (G4 form), Ki: 7 nM |
98% | |||||||||||||||||
Galanthamine HBr |
++
AChE, IC50: 0.35 μM |
98% | |||||||||||||||||
Trospium chloride | ✔ | 99% | |||||||||||||||||
Tiotropium Bromide Monohydrate | ✔ | 97% | |||||||||||||||||
Gallamine Triethiodide |
+
AChR, IC50: 68.0 μM |
98% | |||||||||||||||||
Hexamethonium Bromide | ✔ | 99% | |||||||||||||||||
Pancuronium dibromide | ✔ | 98% | |||||||||||||||||
Neostigmine bromide | ✔ | 98% | |||||||||||||||||
Orphenadrine citrate | ✔ | 98% | |||||||||||||||||
Oxybutynin | ✔ | 98% | |||||||||||||||||
Irsogladine | ✔ | PDE | 99% | ||||||||||||||||
Pyridostigmine bromide | ✔ | 99+% | |||||||||||||||||
Rivastigmine |
+
AChR, IC50: 5.5 μM |
98% | |||||||||||||||||
Paroxetine hydrochloride | ✔ | 99% | |||||||||||||||||
Rocuronium Bromide | ✔ | 98% | |||||||||||||||||
Tropicamide |
+++
M4 mAChR, IC50: 8 nM |
98% | |||||||||||||||||
Diphenmanil methylsulfate | ✔ | 99% | |||||||||||||||||
Umeclidinium bromide | ✔ | 95% | |||||||||||||||||
Otilonium bromide | ✔ | 98% | |||||||||||||||||
Flavoxate HCl |
+
mAChR, IC50: 12.2 μM |
99% | |||||||||||||||||
Ipratropium bromide | ✔ | 98% | |||||||||||||||||
Diphenidol HCl | ✔ | 98% | |||||||||||||||||
Darifenacin hydrobromide |
++++
M3 mAChR, pKi: 8.9 |
98% | |||||||||||||||||
Aclidinium Bromide |
++++
M2 mAChR, Ki: 0.1 nM M4 mAChR, Ki: 0.21 nM |
98% | |||||||||||||||||
Oxybutynin chloride | ✔ | 99% | |||||||||||||||||
Pentoxyverine citrate | ✔ | 98% | |||||||||||||||||
Solifenacin | ✔ | 98% | |||||||||||||||||
Catharanthine | ✔ | 98% | |||||||||||||||||
Benzethonium chloride |
+++
α4β2 nAChRs, IC50: 49 nM α7 nAChRs, IC50: 122 nM |
99+% | |||||||||||||||||
Vinblastine sulfate |
+
nAChR, IC50: 8.9 μM |
99% | |||||||||||||||||
PNU-120596 |
++
α7 nAChR, EC50: 216 nM |
99+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Dronedarone is an amiodarone-like benzofuran which lacks the iodine moiety and presents a methane sulfonyl group that decreases its lipophilicity, thus shortening the half-life and decreasing tissue accumulation. Dronedarone blocks multiple cardiac ion channels and β-adrenoceptors, presenting electrophysiological characteristics of all four Vaughan-Williams classes of antiarrhythmic drugs. Dronedarone was more effective than placebo in maintaining sinus rhythm in patients with paroxysmal and/or persistent AF and was also effective for ventricular rate control during AF (Atrial fibrillation) recurrences, providing incremental rate control on top of standard drugs in permanent AF[3]. Dronedarone decreases the incidence of AF recurrence and the ventricular rate during recurrence. Dronedarone increases mortality in patients with permanent AF and those with moderate-severe heart failure, and should thus be avoided in these populations. Dronedarone is less effective than amiodarone but also has less toxicity[4]. Furthermore, the beneficial effects of oral dronedarone on ventricular rate control were maintained during exercise and sustained with continued therapy. Oral dronedarone was generally well tolerated in the treatment of adult patients with AF and/or atrial flutter in clinical studies[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01288352 | Atrial Fibrillation ... 展开 >> Stroke 收起 << | Phase 4 | Active, not recruiting | November 2019 | Belgium ... 展开 >> 14 Sites Different, Belgium Czech Republic 4 Sites Different, Czech Republic Denmark 2 Sites Different, Denmark France 2 Sites Different, France Germany 51 Sites Different, Germany Italy 12 Sites Different, Italy Netherlands 13 Sites Different, Netherlands Poland 5 Sites Different, Poland Spain 10 Sites Different, Spain Switzerland 5 Sites Different, Switzerland United Kingdom 22 Sites Different, United Kingdom 收起 << |
NCT03607123 | - | Active, not recruiting | July 4, 2022 | China, Jiangsu ... 展开 >> The First Affiliated Hospital of Nanjing Medical University Nanjing, Jiangsu, China, 201129 收起 << | |
NCT00911508 | Atrial Fibrillation ... 展开 >> Arrhythmia 收起 << | Not Applicable | Completed | - | - |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.80mL 0.36mL 0.18mL |
8.98mL 1.80mL 0.90mL |
17.96mL 3.59mL 1.80mL |
CAS号 | 141626-36-0 |
分子式 | C31H44N2O5S |
分子量 | 556.756 |
别名 | SR 33589 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 50 mg/mL(89.81 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |