度洛西汀 T7061

Product Introduction
Bioactivity


英文名: Duloxetine

描述: Duloxetine 是一种 5 羟色胺-去甲肾上腺素重吸收 (serotonin-norepinephrine reuptake) 抑制剂，Ki=4.6 nM，可作用于广泛性焦虑症的研究。

细胞实验: Used the whole cell, patch clamp technique to test whether duloxetine interacts with the neuronal Nav1.7 Na+ channel as a potential target.?Resting and inactivated Nav1.7 Na+ channel block by duloxetine were measured by conventional pulse protocols in transfected human embryonic kidney cells.?The open-channel block was determined directly using inactivation-deficient mutant Nav1.7 Na+ channels[1].

体外活性: IC50 of duloxetine for the resting and inactivated wild-type hNav1.7 Na+ channel were 22.1+/-0.4 and 1.79+/-0.10 microM, respectively (mean+/-SE, n=5).?The IC50 for the open Na+ channel was 0.25+/-0.02 microM (n=5), as determined by the block of persistent late Nav1.7 Na+ currents.?Similar open-channel block by duloxetine was found in the muscle Nav1.4 isoform (IC50=0.51+/-0.05 microM;?n=5).?Block by duloxetine appeared via the conserved local anesthetic receptor as determined by site-directed mutagenesis.?Finally, duloxetine elicited strong use-dependent block of neuronal transient Nav1.7 Na+ currents during repetitive stimulations[1].

存储条件: store at low temperature,store under nitrogenPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 15mg/mL(50.4 mM)


关键字: disorder | depressive | (S)-Duloxetine | SERT | anxiety | inhibit | SLC6A4 | Serotonin Transporter | Inhibitor | musculoskeletal | LY-248686 | generalized | pain | LY 248686 | 5-HTT | osteoarthiritis | LY248686 | Duloxetine

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相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Approved Drug Library | Clinical Compound Library | Antidepressant Compound Library | Neuronal Signaling Compound Library | Inhibitor Library | Pediatric Drug Library | EMA Approved Drug Library | Orally Active Compound Library

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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