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

Ketanserin (Synonyms: R41468)

Cat. No.: HY-10562 Purity: 98.86%
Handling Instructions

Ketanserin is a selective 5-HT 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.

Ketanserin Chemical Structure

Ketanserin Chemical Structure

CAS No. : 74050-98-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 50 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 70 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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Other Forms of Ketanserin:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 0.11 μM (hERG current)[1]
IC50: 152±23 μM (5-HT receptor)[2]

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].

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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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
10 mM 0.2529 mL 1.2644 mL 2.5289 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

Ketanserin is dissolved in DMSO to produce a stock solution of 100 mM. Ketanserin stock is diluted in experimental solutions to achieve the final concentrations[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]

Ketanserin is 0.9% physiological saline group (Rat)[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
Molecular Weight

395.43

Formula

C₂₂H₂₂FN₃O₃

CAS No.

74050-98-9

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 8 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Ketanserin
Cat. No.:
HY-10562
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