1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Serotonin Transporter
  3. Vortioxetine

Vortioxetine (Synonyms: Lu AA 21004)

Cat. No.: HY-15414 Purity: 98.81%
Handling Instructions

Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

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Vortioxetine Chemical Structure

Vortioxetine Chemical Structure

CAS No. : 508233-74-7

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50 mg USD 540 In-stock
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Description

Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

IC50 & Target

sPLA2

15 nM (Ki)

5-HT1B Receptor

33 nM (Ki)

5-HT3A Receptor

3.7 nM (Ki)

Human 5-HT7 Receptor

19 nM (Ki)

SERT

1.6 nM (Ki)

In Vitro

Vortioxetine (Compound 5m) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine displays antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT[1]. Vortioxetine is a partial h5-HT 1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Vortioxetine binds to the r5-HT 7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay[5].

In Vivo

Vortioxetine (Lu AA21004) occupies the r5-HT1B receptor and rSERT (ED50= 3.2 and 0.4 mg/kg, respectively) after subcutaneous administration and is a 5-HT3 receptor antagonist[6]. Vortioxetine significantly increases cell proliferation and cell survival and stimulates maturation of immature granule cells in the sub granular zone of the dentate gyrus of the hippocampus after 21 days of treatment[3]. Vortioxetine does not cause cognitive or psychomotor impairment[4].

Clinical Trial
Molecular Weight

298.45

Formula

C₁₈H₂₂N₂S

CAS No.

508233-74-7

SMILES

CC1=CC=C(SC2=CC=CC=C2N3CCNCC3)C(C)=C1

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 : 50 mg/mL (167.53 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3506 mL 16.7532 mL 33.5064 mL
5 mM 0.6701 mL 3.3506 mL 6.7013 mL
10 mM 0.3351 mL 1.6753 mL 3.3506 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 (8.38 mM); Clear solution

  • 2.

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

    Solubility: 2.5 mg/mL (8.38 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

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

VortioxetineLu AA 21004Lu AA21004Lu AA-210045-HT ReceptorSerotonin TransporterSerotonin Receptor5-hydroxytryptamine Receptor5-HTTSERTSLC6A4Inhibitorinhibitorinhibit

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