2. GPCR/G Protein
    Neuronal Signaling
    Metabolic Enzyme/Protease
  3. Melatonin Receptor
    5-HT Receptor
    Endogenous Metabolite
  4. Agomelatine (L(+)-Tartaric acid)

Agomelatine (L(+)-Tartaric acid)  (Synonyms: S-20098 L(+)-Tartaric acid)

Cat. No.: HY-17038B Purity: 99.82%
COA Handling Instructions

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) 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 L(+)-Tartaric acid 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 (L(+)-Tartaric acid) Chemical Structure

Agomelatine (L(+)-Tartaric acid) Chemical Structure

CAS No. : 824393-18-2

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10 mM * 1 mL in DMSO USD 73 In-stock
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10 mM * 1 mL
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50 mg USD 312 In-stock
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Based on 3 publication(s) in Google Scholar

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Description

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) 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 L(+)-Tartaric acid 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 it 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

393.39

Appearance

Solid

Formula

C19H23NO8
CAS No.
SMILES

CC(NCCC1=C2C=C(OC)C=CC2=CC=C1)=O.O=C(O)[[email protected]](O)[[email protected]@H](O)C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (254.20 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*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 (6.36 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Agomelatine (L(+)-Tartaric acid)824393-18-2S-20098 L(+)-Tartaric acidMelatonin Receptor5-HT ReceptorEndogenous MetaboliteSerotonin Receptor5-hydroxytryptamine ReceptorMT1MT2Agonist5-HT2CAntagonistdepressivedisorderantidepressantInhibitorinhibitorinhibit

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