Ketanserin tartrate
Based on 18 publication(s) in Google Scholar
Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 83846-83-7
- Formula: C26H28FN3O9
- Molecular Weight:545.51
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Ketanserin tartrate
More- J Ethnopharmacol. 2024 Apr 6:323:117703. [Abstract]
- Neurobiol Dis. 2024 Oct 1:200:106651. [Abstract]
- Int J Mol Sci. 2022 Dec 30;24(1):655. [Abstract]
- Pest Manag Sci. 2025 May 13. [Abstract]
- Mol Pain. 2026 Jan-Dec:22:17448069251410452. [Abstract]
- Neuroendocrinology. 2024;114(8):749-774. [Abstract]
- Patent. US20240376052A1.
- Patent. US20240383850A1.
- Patent. US20240279226A1.
- bioRxiv. 2024 Feb 9:2024.02.08.579543. [Abstract]
- bioRxiv. 2024 Jan 20.
- Patent. US20230203070A1.
- University of Cambridge. 2023 Feb.
- Patent. US20220324889A1.
- Patent. US20220289774A1.
- Authorea. September 19, 2022.
- Patent. US20220017549A1.
- Patent. US20220017550A1.
Customer Validation & Images
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT2 Receptor |
hERG current 0.11 μM (IC50) |
Ketanserin tartrate 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 tartrate (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 tartrate 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 83846-83-7
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Appearance Solid
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Molecular Weight 545.51
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Formula C26H28FN3O9
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Color White to off-white
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SMILES
O=C(C1=CC=CC=C1N2)N(CCN3CCC(C(C4=CC=C(F)C=C4)=O)CC3)C2=O.O=C(O)[C@H](O)[C@@H](O)C(O)=O
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Synonyms
R41468 tartrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (18)
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Journal Impact Factor
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Most Recent
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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 -
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 tartrate 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 tartrate 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 tartrate 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 tartrate 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.
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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 tartrate 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.
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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 -
Mol Pain
2026 Jan-Dec:22:17448069251410452. PMID: 41378780 -
Neuroendocrinology
Peripheral 5-HT mediates GnIH-induced feeding behavior and energy metabolism disorder in chickens via the 5-HT2C receptor. [Abstract]2024;114(8):749-774. PMID: 38718758 -
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bioRxiv
Glial expression of Drosophila UBE3A causes spontaneous seizures modulated by 5-HT signaling. [Abstract]2024 Feb 9:2024.02.08.579543. PMID: 38370819 -
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Solvent & Solubility
DMSO : 25 mg/mL (45.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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 (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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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]
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 (sealed storage, away from moisture). 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 | 1.8331 mL | 9.1657 mL | 18.3315 mL | 45.8287 mL |
| 5 mM | 0.3666 mL | 1.8331 mL | 3.6663 mL | 9.1657 mL | |
| 10 mM | 0.1833 mL | 0.9166 mL | 1.8331 mL | 4.5829 mL | |
| 15 mM | 0.1222 mL | 0.6110 mL | 1.2221 mL | 3.0552 mL | |
| 20 mM | 0.0917 mL | 0.4583 mL | 0.9166 mL | 2.2914 mL | |
| 25 mM | 0.0733 mL | 0.3666 mL | 0.7333 mL | 1.8331 mL | |
| 30 mM | 0.0611 mL | 0.3055 mL | 0.6110 mL | 1.5276 mL | |
| 40 mM | 0.0458 mL | 0.2291 mL | 0.4583 mL | 1.1457 mL |
Ketanserin tartrate Related Classifications
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