GLPBio

Quetiapine

Catalog No.: GC14167Purity:>98.00%
COASDSData Sheet
Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine is an atypical antipsychotic used to treat schizophrenia, bipolar disorder, and major depressive disorder.

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Quetiapine
Cas No.: 111974-69-7
10mM (in 1mL DMSO)In Stock
$43.00
1
5mgIn Stock
$24.00
1
10mgIn Stock
$39.00
1
50mgIn Stock
$69.00
1
100mgIn Stock
$84.00
1
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Description

Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine is an atypical antipsychotic used to treat schizophrenia, bipolar disorder, and major depressive disorder[1].

Quetiapine (1, 10μM; 48h) causes cell cycle exit and promotes cell differentiation in primary oligodendrocyte cultures[2].Quetiapine (10, 20, 50μg/mL; 12h) treated had significantly lower levels of MDA and significantly higher activities of SOD and GSH-Px[3].Quetiapine (<100μM; 24h) has no significant effect on cell viabilities[4].

Quetiapine (400 mg/mL; surface application; 0, 6, 12, 24h) treatment significantly reduced skin thickening, erythema and edema, and inflammation caused by UVB irritation. In addition, Quetiapine treatment increased the activity of antioxidant enzymes, including superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), while reducing the production of the oxidised lipid malondialdehyde (MDA)[3].Quetiapine (10, 30, 100mg/kg; po; bid; 28d) elicited a statistically significant, dose-dependent decrease in METH-induced hyperlocomotion 0.5h after administration. There were Quetiapine-induced, dose-dependent decreases in locomotor activity at 8 and 12h[4].

References:
[1].Cross A J, Widzowski D, Maciag C, et al. Quetiapine and its metabolite norQuetiapine: translation from in vitro pharmacology to in vivo efficacy in rodent models[J]. British journal of pharmacology, 2016, 173(1): 155-166.
[2].Mi G, Wang Y, Ye E, et al. The antipsychotic drug Quetiapine stimulates oligodendrocyte differentiation by modulating the cell cycle[J]. Neurochemistry International, 2018, 118: 242-251.
[3]. Xu P, Zhang M, Wang X, et al. Antioxidative effect of Quetiapine on acute ultraviolet-B-induced skin and HaCaT cell damage[J]. International Journal of Molecular Sciences, 2018, 19(4): 953.
[4] Kondo M A, Tajinda K, Colantuoni C, et al. Unique pharmacological actions of atypical neuroleptic Quetiapine: possible role in cell cycle/fate control[J]. Translational psychiatry, 2013, 3(4): e243-e243.

Protocol

Cell experiment [1]:

Cell lines

Human skin keratinocytes cell

Preparation Method

Human skin keratinocytes, HaCaT, were cultured in DMEM supplemented with 10% heat-inactivated fetal bovine serum at 37°C in 5% CO2. The cells were incubated with or without Quetiapine for 12h prior to UVB irradiation. Then, the cells were washed with phosphate buffered saline (PBS; pH7.4) and irradiated using a UVB lamps. The irradiation intensity was monitored by a UVB radiometer. Immediately after UVB irradiation, the cells were returned to the incubator and incubated with drug-free medium for 24h.

Reaction Conditions

10, 20, 50μg/mL; 12h

Applications

The Quetiapine-treated group had significantly lower levels of MDA and significantly higher activities of SOD and GSH-Px compared to the UVB and PBS groups.

Animal experiment [2]:

Animal models

UVB Irradiation Model

Preparation Method

Quetiapine was dissolved in Dimethyl sulfoxide (DMSO) and diluted in phosphate-buffered salt solution (PBS). the working concentration of Quetiapine was the minimum maintenance dose (400mg/mL) used in clinics.Mice were randomly divided into 4 groups that represented treatments or controls. These were: normal healthy controls (no UVB or treatment), UVB irradiation alone (no treatment), UVB irradiation following a sham phosphate buffered saline (PBS) treatment (PBS group), and UVB following Quetiapine treatment (Quetiapine group). Each of these 4 groups was sub-divided randomly into 4 subgroups, which represented various time points to be investigated. Before experimentation, mice were anesthetized by intraperitoneal injection of 1% sodium pentobarbital and hair was removed from the back skin of mice using hair removal wax. Mice were placed 10cm below the lamps, the back skin of mice was collected at 0, 6, 12 and 24h.

Dosage form

400mg/mL; surface application; 0, 6, 12 and 24h

Applications

Quetiapine treatment was able to significantly decrease skin thickness, erythema, and edema, as well as inflammation. Quetiapine treatment increased the activities of antioxidant enzymes, including superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px). In addition, it reduced the production of malondialdehyde (MDA), a kind of oxidized lipid.

References:
[1]. Xu P, Zhang M, Wang X, et al. Antioxidative effect of Quetiapine on acute ultraviolet-B-induced skin and HaCaT cell damage[J]. International Journal of Molecular Sciences, 2018, 19(4): 953.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
111974-69-7
Chemical Name
2-[2-(4-benzo[b][1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol
SMILES
C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42
Molecular Formula
C21H25N3O2S
Molecular Weight
383.51
Solubility
100mg/mL in DMSO（ultrasonic and warming and heat to 45°C), ≥ 29.55 mg/mL in EtOH with gentle warming
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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