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

Ketanserin (tartrate)  (Synonyms: R41468 tartrate; 酒石酸ケタンセリン)

製品番号: HY-10562A 純度: 99.93%
COA 取扱説明書 Technical Support

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).

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CAS 番号 : 83846-83-7

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 60 在庫あり
Solution
10 mM * 1 mL in DMSO USD 60 在庫あり
Solid
50 mg $55 在庫あり
100 mg $77 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 17 publication(s) in Google Scholar

Other Forms of Ketanserin tartrate:

Ketanserin (tartrate) 関連抗体

Top Publications Citing Use of Products

    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.

    Ketanserin tartrate 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.

    5-HT Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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    • 純度とドキュメンテーション

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    製品説明

    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).

    IC50 & Target

    5-HT2 Receptor

     

    hERG current

    0.11 μM (IC50)

    体外実験

    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.

    Ketanserin (tartrate) 関連抗体
    体内実験

    Ketanserin tartrate 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 tartrate 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.
    分子量

    545.51

    分子式

    C26H28FN3O9
    CAS 番号
    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.O=C(O)[C@H](O)[C@@H](O)C(O)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8331 mL 9.1657 mL 18.3315 mL
    5 mM 0.3666 mL 1.8331 mL 3.6663 mL
    10 mM 0.1833 mL 0.9166 mL 1.8331 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 (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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

    V1

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    濃度 （終了）

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    体内:

    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: ≥ 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.
    • Protocol 2

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

    Dosage

    mg/kg

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    (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 (sealed storage, away from moisture)

    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.
    純度とドキュメンテーション

    純度: 99.93%

    COA (252 KB) LCMS (104 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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
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    Ketanserin tartrate Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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      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:

    Ketanserin83846-83-7R41468R 41468R-414685-HT ReceptorPotassium ChannelAutophagySerotonin Receptor5-hydroxytryptamine ReceptorKcsAInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
    HY-10562A
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