决奈达隆 T7056

Product Introduction
Bioactivity


英文名: Dronedarone

描述: Dronedarone (SR 33589) 是一种胺碘酮类似物，对治疗心房颤动可能有效。它是CYP3A4的底物和中度抑制剂。它是多种离子电流的有效阻滞剂，通过非竞争性结合到肾上腺素能受体显示出抗肾上腺素能的效果。

体外活性: Dronedarone reduces the incidence of early and delayed after depolarizations evoked by 1 mM Dofetilide and 0.2 mM Strophantidine in Purkinje fibres. Dronedarone (10 mM) markedly reduces the L-type calcium current (76.5%) and the rapid component of the delayed rectifier potassium current (97%) in ventricular myocytes [1]. Dronedarone inhibits the activity of I(K(ACh)) channels recorded from cell-attached patches by reducing the channel open probability (from 0.56 to 0.11) without modification of the single-channel conductance in single cells isolated from sinoatrial node (SAN) tissue of rabbit hearts [2]. Dronedarone exhibits a state-dependent inhibition of the fast Na(+) channel current with an IC50 of 0.7 μM in guinea pig ventricular myocytes, when the holding potential (V (hold)) is -80 mV. Dronedarone blocks Ca(2+) currents elicited by rectangular pulses at V (hold)?=?-40 mV with IC50 value of 0.4 μM, whereas at V (hold)?=?-80 mV, Dronedarone (10 μM) blocks only 20?% of the current [3].

体内活性: Dronedarone 在正常大鼠心脏中增加动作电位持续时间。Dronedarone 通过69%降低了持续晚期K(+)电流，I(K)（或Isus）。Dronedarone 仅引起I(K)的弱增加I(to)在心肌梗塞后的大鼠中稍有增加[4]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (89.81 mM)


关键字: inoatrial nodal | atrial myocyte | Adrenergic Receptor | Beta Receptor | SR33589 | Cytochrome P450 | atrial flutter | inhibit | Ca channels | mAChR | Inhibitor | Na channels | Autophagy | coronary perfusion | Dronedarone | CYPs | Muscarinic acetylcholine receptor | Calcium Channel | Na+ channels | Sodium Channel | SR-33589 | antiadrenergic | potassium current | Ca2+ channels

相关产品: N-Nornuciferine hydrochloride(4846-19-9 free base) | Ketoconazole | (S)-(+)-N-3-Benzylnirvanol | Schizandrin A | Isocupressic acid | Gomisin G | α-Viniferin | 6',7'-Dihydroxybergamottin | Diflubenzuron | 7-Ethoxyresorufin

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Microbial Natural Product Library

决奈达隆 T7056信息由TargetMol中国为您提供，如您想了解更多关于决奈达隆 T7056报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途