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Purity: = 100%
Agomelatine (S20098; AGO-178; S-20098; AGO178; Valdoxan, Melitor, Thymanax) is a potent and specific agonist of MT1 and MT2 receptors with anti-depressive activity. It has an inverse relationship with the Kis of 0.1, 0.06, 0.12, and 0.27 nM for MT receptor isoforms CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2. Developed to treat major depressive disorder (MDD), it is a special kind of antidepressant. The cloned human 5-HT2A and 5-HT1A exhibit low affinities towards it. Through blocking the inhibitory input of 5-HT2C, agomelatine increases dopamine and noradrenaline levels in in vivo studies.
| Targets |
5-HT2C Receptor ( pKi = 6.4 ); 5-HT2C Receptor ( pKi = 6.2 ); hMT1 ( Ki = 0.1 nM ); hMT1 ( Ki = 0.06 nM ); hMT2 ( Ki = 0.12 nM ); hMT2 ( Ki = 0.27 nM )
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| References |
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| Molecular Formula |
C15H17NO2
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| Molecular Weight |
243.3
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| Exact Mass |
243.13
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| Elemental Analysis |
C, 74.05; H, 7.04; N, 5.76; O, 13.15
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| CAS # |
138112-76-2
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| Related CAS # |
Agomelatine hydrochloride; 1176316-99-6; Agomelatine (L(+)-Tartaric acid); 824393-18-2; Agomelatine-d6; 1079389-42-6; Agomelatin-d3; 1079389-38-0; Agomelatine-d4; 1079389-44-8
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| Appearance |
Solid powder
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| SMILES |
CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC
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| InChi Key |
YJYPHIXNFHFHND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H17NO2/c1-11(17)16-9-8-13-5-3-4-12-6-7-14(18-2)10-15(12)13/h3-7,10H,8-9H2,1-2H3,(H,16,17)
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| Chemical Name |
N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide
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| Synonyms |
S20098; Valdoxan; Thymanax; Melitor; AGO 178; N-(2-(7-methoxy-1-naphthyl)ethyl)acetamide; S 20098; AGO-178; AGO178; S-20098
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1102 mL | 20.5508 mL | 41.1015 mL | |
| 5 mM | 0.8220 mL | 4.1102 mL | 8.2203 mL | |
| 10 mM | 0.4110 mL | 2.0551 mL | 4.1102 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05426304 | Not yet recruiting | Drug: Agomelatine Drug: Placebo Tablets |
Depression Acute Ischemic Stroke |
First Affiliated Hospital, Sun Yat-Sen University |
October 1, 2022 | Phase 4 |
| NCT01822418 | Completed | Drug: agomelatine | Schizophrenia Delusional Disorder |
Central Institute of Mental Health, Mannheim |
January 2013 | Phase 4 |
| NCT01531309 | Completed | Drug: AGO178 | Hepatic Impairment | Novartis Pharmaceuticals | February 8, 2011 | Phase 1 |
| NCT01110902 | Completed | Drug: Placebo Drug: Agomelatine (AGO178C) |
Major Depressive Disorder | Novartis Pharmaceuticals | May 2010 | Phase 3 |
| NCT00411099 | Completed | Drug: agomelatine Drug: placebo |
Major Depressive Disorder | Novartis | December 2006 | Phase 3 |
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