Cat. No.: HY-10562

Ketanserin

(Synonyms: R41468)

17 Cited Publications

Customer Review

Based on 17 publication(s) in Google Scholar

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

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

Purity: 99.89%
CAS No.: 74050-98-9
Formula: C₂₂H₂₂FN₃O₃
Molecular Weight:395.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ketanserin Chemical Structure

CAS No.: 74050-98-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (17)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

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

IC₅₀ & Target

5-HT₂ Receptor

hERG current

0.11 μM (IC₅₀)

All 5-HT Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
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	>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	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	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-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	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	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]
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]
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	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]
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]

In Vitro

Ketanserin at 0.3 μM inhibits the voltage-dependent step current (I_hERG.step) and tail current (I_hERG.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.

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-HT_2A 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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 74050-98-9
Appearance Solid
Molecular Weight 395.43
Formula C₂₂H₂₂FN₃O₃
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
Synonyms

R41468
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

Publications (17)

All Bio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Neurobiol Dis

Glial expression of Drosophila UBE3A causes spontaneous seizures that can be modulated by 5-HT signaling. [Abstract]

2024 Oct 1:200:106651. PMID: 39197537

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.
J Ethnopharmacol

Phytomedicine Fructus Aurantii-derived two absorbed compounds unlock antidepressant and prokinetic multi-functions via modulating 5-HT3/GHSR. [Abstract]

2024 Apr 6:323:117703. PMID: 38185260
Int J Mol Sci

Identification and Pharmacological Characterization of Two Serotonin Type 7 Receptor Isoforms from Mythimna separata. [Abstract]

2022 Dec 30;24(1):655. PMID: 36614100

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

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

Pharmacological characterization and functional roles of the 5-HT7 receptor for pheromone sensitivity and mating in Helicoverpa armigera. [Abstract]

2025 May 13. PMID: 40364570
Neuroendocrinology

Peripheral 5-HT mediates GnIH-induced feeding behavior and energy metabolism disorder in chickens via the 5-HT2C receptor. [Abstract]

2024 May 8. PMID: 38718758
Patent

US20240376052A1.
Patent

US20240383850A1.
Patent

US20240279226A1.
bioRxiv

Glial expression of Drosophila UBE3A causes spontaneous seizures modulated by 5-HT signaling. [Abstract]

2024 Feb 9:2024.02.08.579543. PMID: 38370819
bioRxiv

2024 Jan 20.
Patent

US20230203070A1.
University of Cambridge

2023 Feb.
Patent

US20220324889A1.
Patent

US20220289774A1.
Authorea

September 19, 2022.
Patent

US20220017549A1.
Patent

US20220017550A1.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5289 mL

12.6445 mL

25.2889 mL

5 mM

0.5058 mL

2.5289 mL

5.0578 mL

10 mM

0.2529 mL

1.2644 mL

2.5289 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 1.67 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 (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMF 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.5 mg/mL (1.26 mM); Clear solution

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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 (I_Ks) 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].

MedChemExpress (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-HT_1A receptor agonist (8-OH-DPAT) PS group (DPAT-PS group, n=30); 5-HT_1A receptor antagonist (MDL73005) PS group (MDL-PS group, n=30); 5-HT_2A receptor agonist (DOI) PS group (DOI-PS group, n=30); 5-HT_2A 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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (479 KB)
- 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)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tang Q, et al. The 5-HT2 antagonist Ketanserin is an open channel blocker of human cardiac ether-à-go-go-related gene (hERG) potassium channels. Br J Pharmacol. 2008 Oct;155(3):365-73. [Content Brief]

[2]. Khan N, et al. Investigation of cyclooxygenase and signaling pathways involved in human platelet aggregation mediated by synergistic interaction of various agonists. Drug Des Devel Ther. 2015 Jul 6;9:3497-506. [Content Brief]

[3]. Kekewska A, et al. Antiserotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells. J Pharmacol Exp Ther. 2012 Feb;340(2):369-76. [Content Brief]

[4]. Jiang DG, et al. Serotonin regulates brain-derived neurotrophic factor expression in select brain regions during acute psychological stress. Neural Regen Res. 2016 Sep;11(9):1471-1479. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Ketanserin

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Publications Citing Use of MedChemExpress (MCE) Ketanserin

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Publications (17)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ketanserin Related Classifications

Cat. No.: HY-10562