2. Metabolic Enzyme/Protease GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. Drug Metabolite 5-HT Receptor HCN Channel Serotonin Transporter
  4. Norquetiapine

Norquetiapine  (Synonyms: N-Desalkylquetiapine)

Cat. No.: HY-W052508 Purity: 99.95%
COA
SDS
Handling Instructions Technical Support

Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.

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

Norquetiapine

Norquetiapine Chemical Structure

CAS No. : 5747-48-8

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Norquetiapine:

Norquetiapine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Norquetiapine

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation[1][2][3][4][5].

IC50 & Target

5-HT1A Receptor

 

5-HT2C Receptor

 

5-HT7 Receptor

 

In Vitro

Norquetiapine (5 μM) blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner [1].
Norquetiapine (10-30 μM, 7.5-30 min) selectively inhibits HCN1 currents in Xenopus laevis oocytes by shifting the voltage-dependence of activation to more hyperpolarized potentials and slowing channel opening, with an IC50 of 13.9 μM[2].
Norquetiapine (30 μM, 7.5-15 min) inhibits HCN4 channels in Xenopus laevis oocytes with reduced efficacy compared to HCN1 and has no significant effect on HCN2 channels[2].
Norquetiapine (30 μM, 7.5 min) inhibits HCN1 channels primarily from the closed state in Xenopus laevis oocytes, with minimal effect on open-state channels[2].
Norquetiapine exhibits varying affinities for multiple receptors and the norepinephrine transporter (NET) with Ki values as follows: 196 nM for D2, 48 nM for 5-HT2A, 107 nM for 5-HT2C, 45 nM for 5-HT1A, 76 nM for 5-HT7, 3.5 nM for H1, 144 nM for Alpha-1, 237 nM for Alpha-2, and 58 nM for NET[4].

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

Norquetiapine Related Antibodies
In Vivo

Norquetiapine (10 mg/kg, i.p., once daily, 14 days) shows partial anti-inflammatory effects on IL-10 and IFN-γ in serum and brain following acute LPS challenge in male C57BL/6 mice[3].
Norquetiapine (0.1-1.0 mg/kg, i.p., daily, 12-14 days) displays potent antidepressant-like activity in VMAT2 heterozygous mice[5].

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

Animal Model: Male C57BL/6 mice (2 months old) were injected with LPS(1 mg/kg)[3]
Dosage: 10 mg/kg
Administration: i.p. once daily for 14 days
Result: Increased serum IL-10 levels and decreased serum IFN-γ levels at 4 h post-LPS challenge.
Showed similar regulatory effects on hippocampal IL-10 and IFN-γ gene expression at 4 h post-LPS.
Led to increased IL-1β expression in the PFC at 4 h post-LPS.
Attenuated the increased Il-10 in different brain regions at 24 h post-LPS.
Had no significant effect on LPS-induced changes in anhedonia and short-term recognition memory.
Animal Model: C57BL6 VMAT2 mice (with transmembrane 3 and 4 regions deleted)[5]
Dosage: 0.1, 0.5, 1.0 mg/kg
Administration: i.p. daily for 12 or 14 days
Result: Reduced immobility time in VMAT2 heterozygous mice in the tail suspension test at doses as low as 0.1 mg/kg after acute administration.
Decreased immobility time in VMAT2 heterozygous mice in the tail suspension test following 14-day administration of 0.5 mg/kg.
Showed no significant effect on locomotor activity in both wild-type and VMAT2 heterozygous mice in open-field tests after acute or 14-day administration.
Molecular Weight

295.41

Formula

C17H17N3S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

C12=CC=CC=C1N=C(C3=CC=CC=C3S2)N4CCNCC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (338.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3851 mL 16.9256 mL 33.8511 mL
5 mM 0.6770 mL 3.3851 mL 6.7702 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

SDS (393 KB)

COA (261 KB) HNMR (272 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3851 mL 16.9256 mL 33.8511 mL 84.6279 mL
5 mM 0.6770 mL 3.3851 mL 6.7702 mL 16.9256 mL
10 mM 0.3385 mL 1.6926 mL 3.3851 mL 8.4628 mL
15 mM 0.2257 mL 1.1284 mL 2.2567 mL 5.6419 mL
20 mM 0.1693 mL 0.8463 mL 1.6926 mL 4.2314 mL
25 mM 0.1354 mL 0.6770 mL 1.3540 mL 3.3851 mL
30 mM 0.1128 mL 0.5642 mL 1.1284 mL 2.8209 mL
40 mM 0.0846 mL 0.4231 mL 0.8463 mL 2.1157 mL
50 mM 0.0677 mL 0.3385 mL 0.6770 mL 1.6926 mL
60 mM 0.0564 mL 0.2821 mL 0.5642 mL 1.4105 mL
80 mM 0.0423 mL 0.2116 mL 0.4231 mL 1.0578 mL
100 mM 0.0339 mL 0.1693 mL 0.3385 mL 0.8463 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Norquetiapine Related Classifications

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.

Keywords:

Norquetiapine5747-48-8N-DesalkylquetiapineDrug Metabolite5-HT ReceptorHCN ChannelSerotonin TransporterSerotonin Receptor5-hydroxytryptamine ReceptorHyperpolarization activated cyclic nucleotide gated channels5-HTTSERTSLC6A45-HTNETdepressionimmunologyInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Norquetiapine
Cat. No.:
HY-W052508
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Portuguese - PT (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.