2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Autophagy
  3. 5-HT Receptor Potassium Channel Autophagy
  4. Ketanserin

Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).

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

CAS No. : 74050-98-9

Size Price Stock Quantity
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
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 17 publication(s) in Google Scholar

Other Forms of Ketanserin:

Ketanserin Related Antibodies

Top Publications Citing Use of Products

    Ketanserin purchased from MedChemExpress. Usage Cited in: Neurobiol Dis. 2024 Oct 1:200:106651.  [Abstract]

    Representative activity patterns were determined by HMC in control-diet repo > w1118 flies, and repo > dube3a flies fed Ketanserin (KET) (0.4 μM).

    Ketanserin purchased from MedChemExpress. Usage Cited in: Neurobiol Dis. 2024 Oct 1:200:106651.  [Abstract]

    Ketanserin (KET) (0.04-0.4 μM) decreased immobilization time and the rate of high-velocity events of repo > dube3a flies during the high-temperature period.

    Ketanserin purchased from MedChemExpress. Usage Cited in: Neurobiol Dis. 2024 Oct 1:200:106651.  [Abstract]

    Representative traces of DLM spiking in repo > dube3a flies treated with Ketanserin (KET) (0.04-0.4 μM) compared to repo > dube3a and repo > w1118 flies reared on the control diet.

    Ketanserin purchased from MedChemExpress. Usage Cited in: Neurobiol Dis. 2024 Oct 1:200:106651.  [Abstract]

    Ketanserin (KET) (0.04-0.4 μM) reduced overall firing frequency and bursting in repo > dube3a flies.

    Ketanserin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Dec 30;24(1):655.

    Ketanserin (40 μM) decreased the 5-HT induced response in HEK293 cells expressing Msep5-HT7L or Msep5-HT7S receptors.

    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

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).

    IC50 & Target

    5-HT2 Receptor

     

    hERG current

    0.11 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    260 nM
    Compound: Ketanserin
    Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
    Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
    		[PMID: 9357514]
    CHO IC50
    270 nM
    Compound: 7
    Displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells
    Displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells
    		[PMID: 10585208]
    CHO IC50
    6500 nM
    Compound: Ketanserin
    Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
    Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
    		[PMID: 9357514]
    CHO IC50
    > 10000 nM
    Compound: 7
    Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
    Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
    		[PMID: 10585208]
    CHO-K1 IC50
    0.29 μM
    Compound: ketanserin
    Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
    Displacement of [3H]Lysergic acid from human recombinant 5HT2B receptor expressed in CHOK1 cells after 60 mins
    		[PMID: 23403082]
    CHO-K1 IC50
    11 nM
    Compound: Ketanserin
    Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
    Antagonist activity against human recombinant 5-HT2A receptor expressed in CHOK1 cells assessed as reduction in alpha-methylserotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
    		[PMID: 25557493]
    CHO-K1 IC50
    32 nM
    Compound: Ketanserin
    Antagonist activity at human 5HT2A receptor expressed in EC80 serotonin-stimulated CHOK1 cells by calcium mobilization assay
    Antagonist activity at human 5HT2A receptor expressed in EC80 serotonin-stimulated CHOK1 cells by calcium mobilization assay
    		[PMID: 19328689]
    CHO-K1 IC50
    80 nM
    Compound: Ketanserin
    Antagonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay
    Antagonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay
    		[PMID: 23675993]
    HEK293 EC50
    1.04 nM
    Compound: Ketanserin
    Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
    Antagonist activity at serotonin-activated human recombinant 5HT-2A receptor expressed in HEK293 cells assessed as decrease in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
    		[PMID: 23537943]
    HEK293 IC50
    0.52 nM
    Compound: Ketanserin
    Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor in HEK293 cells after 60 mins by scintillation counting
    Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor in HEK293 cells after 60 mins by scintillation counting
    		[PMID: 27997171]
    HEK293 IC50
    3.5 x 10-10 M
    Compound: Ketanserin
    Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEK293 cells
    Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEK293 cells
    		[PMID: 26988801]
    HEK293 IC50
    3.5 x 10-10 M
    Compound: Ketanserin
    Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
    Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
    		[PMID: 27876250]
    In Vitro

    Ketanserin at 0.3 μM inhibits the voltage-dependent step current (IhERG.step) and tail current (IhERG.tail) of hERG channels with a 5-min exposure[1]. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC50=22.0±7 μM), Ketanserin (IC50=152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC50 value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM[2]. Ketanserin inhibits platelet aggregation with an IC50 of 240 (169-339) nM[3].

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

    Ketanserin Related Antibodies
    In Vivo

    Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions[4].

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

    395.43

    Formula

    C22H22FN3O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=CC=C1N2)N(CCN3CCC(C(C4=CC=C(F)C=C4)=O)CC3)C2=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 16.67 mg/mL (42.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    DMF : 5 mg/mL (12.64 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5289 mL 12.6445 mL 25.2889 mL
    5 mM 0.5058 mL 2.5289 mL 5.0578 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (4.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 1.67 mg/mL (4.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 6.25 mg/mL (15.81 mM); Suspended solution; Need ultrasonic

    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).
    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: 99.89%

    SDS (479 KB)

    COA (246 KB) HNMR (263 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    The established HEK 293 cell line stably expressing hERG channels is cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% foetal bovine serum, 400 μg/mL G418. The HEK 293 cell line stably expressing recombinant human cardiac KCNQ1/KCNE1 channel current (IKs) is maintained in DMEM containing 10% foetal bovine serum and 100 μg/mL hygromycin. Cells used for electrophysiology are seeded on a glass coverslip. The mutant hERG channels are constructed, and are transiently expressed in HEK 293 cells using 10 μL of Lipofectamine 2000 with 4 μg of hERG mutant cDNA in pCDNA3 vector[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Rat[4]
    A total of 155 specific-pathogen-free 2-month-old male Sprague-Dawley rats, weighing 180-220 g, are used. The rats are randomly divided into the following six groups: 5-HT1A receptor agonist (8-OH-DPAT) PS group (DPAT-PS group, n=30); 5-HT1A receptor antagonist (MDL73005) PS group (MDL-PS group, n=30); 5-HT2A receptor agonist (DOI) PS group (DOI-PS group, n=30); 5-HT2A receptor antagonist (Ketanserin) PS group (Ketan-PS group, n=30); the solvent control no-stress group (0.9% physiological saline group, CON group); and the PS only group (PS group, n=30). The DPAT-PS, MDL-PS, DOI-PS, Ketan-PS and PS groups are further divided into six subgroups (n=5 each) according to the time between the stress and analysis; immediately after stress, and 0.5, 1, 2, 6 and 24 hours after stress. The CON group (n=5) receive normal feed. For the Ketan-PS group, Ketanserin, dissolved in 0.9% physiological saline, is injected intraperitoneally at 5 mg/kg at 1 hour before each stress exposure.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMF / DMSO 1 mM 2.5289 mL 12.6445 mL 25.2889 mL 63.2223 mL
    5 mM 0.5058 mL 2.5289 mL 5.0578 mL 12.6445 mL
    10 mM 0.2529 mL 1.2644 mL 2.5289 mL 6.3222 mL
    DMSO 15 mM 0.1686 mL 0.8430 mL 1.6859 mL 4.2148 mL
    20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1611 mL
    25 mM 0.1012 mL 0.5058 mL 1.0116 mL 2.5289 mL
    30 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1074 mL
    40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5806 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.

    Ketanserin 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:

    Ketanserin74050-98-9R41468R 41468R-414685-HT ReceptorPotassium ChannelAutophagySerotonin Receptor5-hydroxytryptamine ReceptorKcsAInhibitorinhibitorinhibit

    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:
    Ketanserin
    Cat. No.:
    HY-10562
    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 (479 KB) Français - FR (479 KB) Deutsch - DE (479 KB) Norwegian - NO (479 KB) Español - ES (479 KB) Swedish - SV (479 KB) Italian - IT (479 KB) Korean - KR (479 KB) Portuguese - PT (479 KB)

    Request for HNMR Report

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