Agomelatine | S-20098 | MT1/2 Agonist | AmBeed-信号通路专用抑制剂

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阿戈美拉汀 /Agomelatine {[allProObj[0].p_purity_real_show]}

货号：A643275 同义名： S-20098

Agomelatine is a melatonin structurely similar 5-HT2C receptor antagonist as well as a potent melatonin receptor agonist, used to treat major depressive disorder.

Agomelatine 化学结构
CAS号：138112-76-2

Agomelatine 3D分子结构
CAS号：138112-76-2

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Agomelatine 纯度/质量文件产品仅供科研

货号：A643275 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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5-羟色胺受体亚型比较

产品名称	5-HT ↓ ↑	5-HT1 ↓ ↑	5-HT2 ↓ ↑	5-HT3 ↓ ↑	5-HT5 ↓ ↑	5-HT6 ↓ ↑	5-HT7 ↓ ↑	其他靶点	纯度
Desvenlafaxine	++ 5-HT, Ki: 40.2 nM								98%
Lamotrigine	+ 5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM								98%
Venlafaxine	✔								98%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								98%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	98%
Fluoxetine HCl	✔								99.5%
Paroxetine hydrochloride	✔							AChR	97%
BMY 7378		++ 5-HT1D, pIC50: 5.9 5-HT1A, pIC50: 6.4	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						98%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						98% HPLC
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Rat), Ki: 50 nM 5-HT2C (Human), Ki: 2.5 nM						99%+
Loxapine succinate			++ 5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM						99%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					98%
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
Asenapine maleate		+++ 5-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 5-HT2C, pKi: 10.46 5-HT2A, pKi: 9.75		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		97%
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 5-HT2B, pKi: 6.2 5-HT2A, pKi: 6.6			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
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。

Agomelatine 生物活性

靶点

5-HT2

描述

Agomelatine behaves both as a potent agonist at melatonin MT1 and MT2 receptors and as a neutral antagonist at 5-HT2C receptors. Agomelatine dose-dependently inhibits the firing of cells in the SCN (the endogeneous master clock) in Syrian hamsters (ED50 = 0.91 mg/kg, i.p.)^[3]. In CSDS (chronic social defeat stress) mice treated 3 weeks with 50 mg/kg/d agomelatine, the anxious-like phenotype was not reversed, but the treatment successfully prevented the cognitive impairments and hippocampal gene expression modifications^[4].

Agomelatine 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
CHO cells		Function assay	120 mins	Displacement of [125I]iodomelatonin form human MT1 receptor expressed in CHO cells after 120 mins, Ki=0.1 nM	22301214
CHO-Galpha16 cells		Function assay	20 mins	Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=2.1 nM	21237644
HEK 293		Function assay		Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=6e-05 μM	12646022

Agomelatine 参考文献

[1]Dagytė G, Crescente I, et al. Agomelatine reverses the decrease in hippocampal cell survival induced by chronic mild stress. Behav Brain Res. 2011 Mar 17;218(1):121-8.

[2]Zajecka J, Schatzberg A, et al. Efficacy and safety of agomelatine in the treatment of major depressive disorder: a multicenter, randomized, double-blind, placebo-controlled trial. J Clin Psychopharmacol. 2010 Apr;30(2):135-44.

[3]Guardiola-Lemaitre B, De Bodinat C, Delagrange P, Millan MJ, Munoz C, Mocaër E. Agomelatine: mechanism of action and pharmacological profile in relation to antidepressant properties. Br J Pharmacol. 2014 Aug;171(15):3604-19. doi: 10.1111/bph.12720. PMID: 24724693; PMCID: PMC4128060.

[4]Martin V, Allaïli N, Euvrard M, Marday T, Riffaud A, Franc B, Mocaër E, Gabriel C, Fossati P, Lehericy S, Lanfumey L. Effect of agomelatine on memory deficits and hippocampal gene expression induced by chronic social defeat stress in mice. Sci Rep. 2017 Apr 4;8:45907. doi: 10.1038/srep45907. PMID: 28374847; PMCID: PMC5379201.

Agomelatine 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

4.11mL

0.82mL

0.41mL

20.55mL

4.11mL

2.06mL

41.10mL

8.22mL

4.11mL

Agomelatine 技术信息

CAS号	138112-76-2
分子式	C₁₅H₁₇NO₂
分子量	243.301

别名	S-20098
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(431.56 mM)，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

动物实验配方

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Agomelatine 生物活性

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Agomelatine 参考文献

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全球学术期刊中引用的产品

Agomelatine 质控信息

Agomelatine 生物活性

Agomelatine 细胞研究

Agomelatine 参考文献

Agomelatine 实验方案

Agomelatine 技术信息

最近浏览的产品

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