Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
Other Sizes |
|
Purity: ≥98%
Quetiapine Fumarate (also known as ICI-204636; trade name Seroquel) is a dibenzothiazepine-based atypical antipsychotic agent acting as a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. It has been authorized for use in the management of bipolar I and II depression, schizophrenia, and bipolar I mania. It is possible that antagonist activity at serotonin and dopamine receptors mediates quetiapine's antipsychotic effect. Particularly, quetiapine inhibited the alpha 1 and alpha 2 adrenoreceptors, the 5-HT1A and 5-HT2 serotonin receptor subtypes, and the D1 and D2 dopamine receptors.
Targets |
5-HT1a Receptor ( pKi = 5.74 ); 5-HT2A Receptor ( pKi = 7.54 ); 5-HT2C Receptor ( pKi = 5.55 ); D2 Receptor ( pKi = 7.25 ); 5-HT1A Receptor ( pKi = 4.77 ); D2 Receptor ( pKi = 6.33 )
|
---|---|
ln Vitro |
Quetiapine (<100 μM; 24 hours) has no significant effect on cell viability [2]. Quetiapine (10 μM) inhibits NO release, while LPS (0.1-100 ng/mL) concentration modulates [2]. Cell viability assay [2] Cell line: N9 microglia Concentration: 0, 0.1, 1, 10, 50 and 100 μM Incubation time: 24 hours Results: No significant effect on cells. viability at various concentrations below 100 μM, where significant toxicity was observed. RT-PCR[2] Cell line: N9 microglia Concentration: 10 μM Incubation time: 24 hours Results: Significantly inhibited TNF-α synthesis.
|
ln Vivo |
Quetiapine (10 mg/kg/day; approved) can attenuate the recruitment and activation of astrocytes and promote myelin repair in a cuprizone (CPZ)-induced chronic demyelination model [2]. Animal model: C57BL/ 6 mice [2] Dosage: 10 mg/kg/day Administration method: Ingestion Results: Compared with the Veh group, the optical density of myelin basic protein (MBP) staining increased significantly.
|
Cell Assay |
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. |
Animal Protocol |
C57BL/6 mice
10 mg/kg/day Ingested |
References |
|
Molecular Formula |
C21H25N3O2S
|
---|---|
Molecular Weight |
383.51
|
Exact Mass |
383.17
|
Elemental Analysis |
C, 65.77; H, 6.57; N, 10.96; O, 8.34; S, 8.36
|
CAS # |
111974-69-7
|
Related CAS # |
Quetiapine hemifumarate; 111974-72-2; Quetiapine sulfoxide dihydrochloride;329218-11-3; Quetiapine-d4 fumarate; 1287376-15-1; Quetiapine sulfoxide; 329216-63-9; 918505-61-0 (analog)
|
Appearance |
Oil
|
SMILES |
C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42
|
InChi Key |
URKOMYMAXPYINW-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2
|
Chemical Name |
2-[2-(4-benzo[b][1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol
|
Synonyms |
ICI 204636; ICI-204636; ICI 204,636; ICI204636; Quetiapine; quetiapine fumarate; brand name: Seroquel
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: 77~100 mg/mL (200.8~260.8 mM)
Ethanol: ~100 mg/mL (~260.8 mM) H2O: ~0.1 mg/mL (~0.3 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6075 mL | 13.0375 mL | 26.0749 mL | |
5 mM | 0.5215 mL | 2.6075 mL | 5.2150 mL | |
10 mM | 0.2607 mL | 1.3037 mL | 2.6075 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04521478 | Active Recruiting |
Drug: BI 1358894 Drug: Placebo Drug: Quetiapine |
Depressive Disorder, Major | Boehringer Ingelheim | November 20, 2020 | Phase 2 |
NCT05801289 | Recruiting | Drug: Quetiapine | Delirium | Ain Shams University | December 4, 2022 | Not Applicable |
NCT05085808 | Not yet recruiting | Drug: Quetiapine Drug: Placebo |
Morality Delirium Psych |
University of Southern California | March 1, 2024 | Phase 4 |
NCT05240261 | Not yet recruiting | Drug: Quetiapine | Chronic Kidney Diseases | Assiut University | May 1, 2022 | Phase 1 |
NCT05480150 | Recruiting | Drug: Quetiapine Fumarate Tablets Drug: Lurasidone |
Major Depressive Disorder Bipolar Disorder, Mixed |
First Affiliated Hospital of Zhejiang University |
November 1, 2021 | Not Applicable |
Occupancy of rat noradrenline transporter (NET) in locus coeruleus following s.c. administration of norquetiapine, desipramine or reboxetine. Br J Pharmacol . 2016 Jan;173(1):155-66. td> |
Effects of norquetiapine, desipramine or reboxetine in the forced swim test in male BALB/c mice. Br J Pharmacol . 2016 Jan;173(1):155-66. td> |