1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor
  3. Quetiapine hemifumarate

Quetiapine hemifumarate 

Cat. No.: HY-B0031 Purity: 98.24%
Handling Instructions

Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.

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

Quetiapine hemifumarate Chemical Structure

Quetiapine hemifumarate Chemical Structure

CAS No. : 111974-72-2

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Based on 1 publication(s) in Google Scholar

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Description

Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].

IC50 & Target[1]

5-HT1A Receptor

5.74 (pKi)

5-HT2A Receptor

7.54 (pKi)

5-HT2C Receptor

5.55 (pKi)

D2 Receptor

7.25 (pKi)

5-HT1A Receptor

4.77 (pEC50)

D2 Receptor

6.33 (pIC50)

In Vitro

Quetiapine (<100 μM; 24 hours) has no significant effect on cell viabilities[2].
Quetiapine (10 μM) inhibits NO release, which increased by LPS (0.1-100 ng/mL) in concentration-dependent manner[2].
Quetiapine (10 μM) also inhibits TNF-α synthesis[2].

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

Cell Viability Assay[2]

Cell Line: N9 microglial cells
Concentration: 0, 0.1, 1, 10, 50, and 100 μM
Incubation Time: 24 hours
Result: Had no significant effect on cell viabilities at various concentrations under 100 μM, in which significant toxicity could be observed.

RT-PCR[2]

Cell Line: N9 microglial cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Dramatically inhibited TNF-α synthesis.
In Vivo

Quetiapine (10 mg/kg/day; ingested) can alleviate the recruitment and activation of microglia and promote myelin repair in Cuprizone (CPZ)-induced chronic mouse model of demyelination[1].

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

Animal Model: C57BL/6 mice[2]
Dosage: 10 mg/kg/day
Administration: Ingested
Result: Significantly increased in optical density of myelin basic protein (MBP) staining compared to Veh group.
Clinical Trial
Molecular Weight

441.54

Formula

C₂₃H₂₇N₃O₄S

CAS No.

111974-72-2

SMILES

OCCOCCN(CC1)CCN1C2=NC(C=CC=C3)=C3SC4=C2C=CC=C4.O=C(O)/C=C/C(O)=O.[0.5]

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 (113.24 mM; Need ultrasonic)

H2O : 1.25 mg/mL (2.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2648 mL 11.3240 mL 22.6480 mL
5 mM 0.4530 mL 2.2648 mL 4.5296 mL
10 mM 0.2265 mL 1.1324 mL 2.2648 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 (5.66 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

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

Purity: 98.24%

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Keywords:

Quetiapine hemifumarate5-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1AD25-HT2A5-HT2CAntidepressantanxiolyticInhibitorinhibitorinhibit

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