1. GPCR/G Protein
    Neuronal Signaling
  2. Melatonin Receptor
    5-HT Receptor
  3. Agomelatine

Agomelatine (Synonyms: S-20098)

Cat. No.: HY-17038 Purity: 98.77%
Handling Instructions

Agomelatine (S-20098) is 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. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

For research use only. We do not sell to patients.

Agomelatine Chemical Structure

Agomelatine Chemical Structure

CAS No. : 138112-76-2

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10 mM * 1 mL in DMSO USD 73 In-stock
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100 mg USD 396 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Agomelatine (S-20098) is 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[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

IC50 & Target

5-HT2C Receptor

6.4 (pKi, native porcine)

5-HT2C Receptor

6.2 (pKi, human)

hMT1

0.1 nM (Ki, CHO Cells)

hMT1

0.06 nM (Ki, HEK Cells)

hMT2

0.12 nM (Ki, CHO Cells)

hMT2

0.27 nM (Ki, HEK Cells)

In Vitro

Agomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC50s of 1.6±0.4, 0.10±0.04 nM for CHO hMT1, CHO-hMT2 (hΜΤ1 and hΜΤ2 receptors expressed in CHO or HEK cell membranes)[1].
Agomelatine (S20098) also interacts with h5-HT2B receptors (6.6), whereas Agomelatine shows low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors, and negligible (<5.0) affinity for other 5-HT receptors[2].

In Vivo

Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls[3].

Animal Model: 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[3].
Dosage: 25, 50, or 75 mg/kg
Administration: Administered intraperitoneally (i.p.)
Result: All dosages showed a significant decrease in thiobarbituric acid reactive substances (TBARS) levels and nitrite content in all brain areas when compared to controls in the Pilocarpine induced seizure model.
All dosages decreased TBARS levels in all brain areas, and at low doses (25 or 50 mg/kg) decreased nitrite contents, but only at 25 or 50 mg/kg showed a significant increase in catalase activity in three brain areas when compared to controls in the Strychnine-induced seizure model.
Did not have any antioxidant effects on parameters of oxidative stress produced by PTX- or PTZ-induced seizure models when compared to controls.
Clinical Trial
Molecular Weight

243.30

Formula

C₁₅H₁₇NO₂

CAS No.

138112-76-2

SMILES

CC(NCCC1=C2C=C(OC)C=CC2=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (411.02 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.28 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.28 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.28 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AgomelatineS-20098S20098S 20098Melatonin Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorMT1MT2Agonist5-HT2CAntagonistdepressivedisorderantidepressantInhibitorinhibitorinhibit

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