Agomelatine (Synonyms: S20098) |
| رقم الكتالوجGC17981 |
Agomelatine (S-20098) هو ناهض محدد لمستقبلات MT1 و MT2 مع Kis 0.1 و 0.06 و 0.12 و 0.27 نانومتر لـ CHO-hMT1 و HEK-hMT1 و CHO-hMT2 و HEK-hMT2 على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 138112-76-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
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 | |
| المرادفات | S20098 | ||
| Chemical Name | N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide | ||
| Canonical SMILES | CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC | ||
| Formula | C15H17NO2 | M.Wt | 243.3 |
| الذوبان | ≥ 12.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *