Agomelatine
(Synonyms: 阿戈美拉汀; S-20098) 目录号 : GC17981
Agomelatine是一种褪黑素（MT）受体激动剂，对MT1和MT2的Ki值分别为0.1 nM和0.12 nM。Agomelatine也是一种5-羟色胺（5-HT）受体拮抗剂，对5-HT2C 和5-HT2B 的Ki值分别为631 nM和660 nM。
Cas No.:138112-76-2
Sample solution is provided at 25 µL, 10mM.
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Agomelatine is a melatonin (MT) receptor agonist with Ki values of 0.1 nM and 0.12 nM for MT1 and MT2, respectively[1]. Agomelatine is also a 5-hydroxytryptamine (5-HT) receptor antagonist with Ki values of 631 nM and 660 nM for 5-HT2C and 5-HT2B respectively[2]. Agomelatine can regulate circadian rhythm and enhance mood, and is used in research on major depressive disorder (MDD) [3].
In vitro, Agomelatine (10, 20 μM) treated endothelial cells and monocytes for 24 h, dose-dependently inhibited the angiotensin II-induced increase in the expression of AT1R, VCAM-1 and ICAM-1 and reduced cell adhesion [4]. Agomelatine (8, 16 μM) treated hippocampal neuron HT22 cells for 24 hours, inhibited the neurotoxicity caused by cisplatin injury, and attenuated oxidative stress and inflammatory response [5].
In vivo, Agomelatine (40mg/kg) was treated by intraperitoneal injection in rats with LPS-induced depression and significantly improved the rats' anxiety and depression-like behaviors, reducing neuroinflammation and neuronal damage[6]. Agomelatine (25, 50 or 75 mg/kg; ip) has antioxidant activity in a mouse seizure model [7].
References:
[1] Dridi D, Zouiten A, Mansour H B. Depression: chronophysiology and chronotherapy[J]. Biological rhythm research, 2014, 45(1): 77-91.
[2] Millan M J, Gobert A, Lejeune F, et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 306(3): 954-964.
[3] Smeraldi E, Delmonte D. Agomelatine in depression[J]. Expert opinion on drug safety, 2013, 12(6): 873-880.
[4] Hong N, Ye Z, Lin Y, et al. Agomelatine prevents angiotensin II-induced endothelial and mononuclear cell adhesion[J]. Aging (albany NY), 2021, 13(14): 18515.
[5] Cankara F N, Günaydın C, Çelik Z B, et al. Agomelatine confers neuroprotection against cisplatin-induced hippocampal neurotoxicity[J]. Metabolic brain disease, 2021, 36(2): 339-349.
[6] Lan T, Wu Y, Zhang Y, et al. Agomelatine rescues lipopolysaccharide-induced neural injury and depression-like behaviors via suppression of the Gαi-2-PKA-ASK1 signaling pathway[J]. Journal of neuroinflammation, 2022, 19(1): 117.
[7] Aguiar C C T, Almeida A B, Araújo P V P, et al. Effects of agomelatine on oxidative stress in the brain of mice after chemically induced seizures[J]. Cellular and molecular neurobiology, 2013, 33: 825-835.
Agomelatine是一种褪黑素（MT）受体激动剂，对MT1和MT2的Ki值分别为0.1 nM和0.12 nM[1]。Agomelatine也是一种5-羟色胺（5-HT）受体拮抗剂，对5-HT2C 和5-HT2B 的Ki值分别为631 nM和660 nM[2]。Agomelatine可以调节昼夜节律和提升情绪，应用于重度抑郁症（MDD）研究[3]。
在体外，Agomelatine（10、20μM）处理内皮细胞和单核细胞24h，剂量依赖性地抑制了血管紧张素II诱导的AT1R、VCAM-1和ICAM-1的表达增加，减少了细胞粘附[4]。Agomelatine（8、16μM）处理海马神经元HT22细胞24h，抑制了顺铂损伤引起的神经毒性，减弱了氧化应激和炎症反应[5]。
在体内，Agomelatine（40mg/kg）通过腹膜注射治疗LPS诱导的抑郁症大鼠，显著改善了大鼠的焦虑和抑郁样行为，减轻了神经炎症和神经元损伤[6]。Agomelatine (25、50或75 mg/kg；ip) 在小鼠癫痫发作模型中具有抗氧化活性[7]。
Cell experiment [1]: | |
Cell lines | HUVEC cells |
Preparation method | HUVECs were exposed to Ang II (1μM) with or without Agomelatine (10, 20 μM) for 24 h. |
Reaction Conditions | 10, 20 μM; 24 h |
Applications | Introduction of 10 and 20μM Agomelatine prevented the increase in AT1R expression induced by exposure to Ang II, with the higher dose having a more robust inhibitory effect. |
Animal experiment [2]: | |
Animal models | LPS-induced rat model of depression |
Preparation method | Agomelatine was dissolved in 1% hydroxyethyl cellulose (HEC) solution. In all experiments, agomelatine (40mg/kg) was administered via an i.p. injection at 60 min prior to daily LPS procedures. |
Dosage form | 40mg/kg; i.p. |
Applications | Agomelatine can reverse LPS-induced depression-like behavior in rats and reduce the neuroinflammatory response in the DG area of the brain. |
References: [1] Hong N, Ye Z, Lin Y, et al. Agomelatine prevents angiotensin II-induced endothelial and mononuclear cell adhesion[J]. Aging (albany NY), 2021, 13(14): 18515. [2]Lan T, Wu Y, Zhang Y, et al. Agomelatine rescues lipopolysaccharide-induced neural injury and depression-like behaviors via suppression of the Gαi-2-PKA-ASK1 signaling pathway[J]. Journal of neuroinflammation, 2022, 19(1): 117. | |
| Cas No. | 138112-76-2 | SDF | |
| 别名 | 阿戈美拉汀; S-20098 | ||
| 化学名 | N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide | ||
| Canonical SMILES | CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC | ||
| 分子式 | C15H17NO2 | 分子量 | 243.3 |
| 溶解度 | ≥ 12.2mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1102 mL | 20.5508 mL | 41.1015 mL |
| 5 mM | 0.822 mL | 4.1102 mL | 8.2203 mL |
| 10 mM | 0.411 mL | 2.0551 mL | 4.1102 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet