Size | Price | Stock | Qty |
---|---|---|---|
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Agomelatine L(+)-Tartaric acid is a potent antidepressant acting as a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Because Agomelatine L(+)-tartaric acid antagonizes the 5-HT2C receptor, it is categorized as a norepinephrine-dopamine disinhibitor (NDDI). It is an innovative antidepressant designed to treat major depressive disorder (MDD). Its affinities for cloned human 5-HT2A and 5-HT1A are low. In the in vivo experiments, Agomelatine increases noradrenaline and dopamine levels by inhibiting 5-HT2C's inhibitory input.
Targets |
5-HT2C Receptor ( pKi = 6.4 ); 5-HT2C Receptor ( pIC50 = 6.2 ); hMT1 ( Ki = 0.1 nM ); hMT1 ( Ki = 0.06 nM ); hMT2 ( Ki = 0.12 nM );hMT2 ( Ki = 0.27 nM )
|
---|---|
ln Vitro |
Agomelatine (S 20098) functions as a complete agonist for both MT1 and MT2 receptors, with EC50 values of 1.6±0.4 and 0.10±0.04 nM for CHO hMT1 CHO-hMT2 (hΜΤ1 and hΜΤ2 receptors expressed in the membranes of CHO or HEK cells, respectively|1].
Agomelatine (S20098) interacts with h5-HT2B receptors as well (6.6). However, it exhibits negligible (<5.0) affinity for other 5-HT receptors and low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors[2]. |
ln Vivo |
Agomelatine (25, 50, or 75 mg/kg; i.p.) exhibits antioxidant activity in mouse seizure models induced by strychnine (75 mg/kg, i.p.) or pilocarpine (400 mg/kg, i.p.). Comparing the oxidative stress parameters produced by seizure models induced by either picrotoxin (PTX) or pentylenetetrazole (PTZ) to controls, agomelatine dose did not produce any antioxidant effects[3].
|
Animal Protocol |
Female Swiss mice (20-30 g) were administered PTZ (85 mg/kg, i.p.), PTX (7 mg/kg, i.p.), strychnine (75 mg/kg, i.p.), Pilocarpine (400 mg/kg, i.p.), respectively
25, 50, or 75 mg/kg Administered intraperitoneally (i.p.) |
References |
|
Molecular Formula |
C19H23NO8
|
---|---|
Molecular Weight |
393.3878262043
|
Exact Mass |
393.14
|
CAS # |
824393-18-2
|
Related CAS # |
Agomelatine; 138112-76-2; Agomelatine hydrochloride; 1176316-99-6
|
Appearance |
Powder
|
SMILES |
CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
|
InChi Key |
PJOPJXPTFZIKTL-LREBCSMRSA-N
|
InChi Code |
InChI=1S/C15H17NO2.C4H6O6/c1-11(17)16-9-8-13-5-3-4-12-6-7-14(18-2)10-15(12)13;5-1(3(7)8)2(6)4(9)10/h3-7,10H,8-9H2,1-2H3,(H,16,17);1-2,5-6H,(H,7,8)(H,9,10)/t;1-,2-/m.1/s1
|
Chemical Name |
(2R,3R)-2,3-dihydroxybutanedioic acid;N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide
|
Synonyms |
S-20098 L(+)-Tartaric acid; Agomelatine (L(+)-Tartaric acid)
|
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)
|
Solubility (In Vitro) |
DMSO: ~100 mg/mL (~254.2 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.36 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (6.36 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 (6.36 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 | 2.5420 mL | 12.7100 mL | 25.4201 mL | |
5 mM | 0.5084 mL | 2.5420 mL | 5.0840 mL | |
10 mM | 0.2542 mL | 1.2710 mL | 2.5420 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.