2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. 5-HT Receptor Histamine Receptor Dopamine Receptor Adrenergic Receptor
  4. Ritanserin

Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.

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

Ritanserin Chemical Structure

Ritanserin Chemical Structure

CAS No. : 87051-43-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 3 publication(s) in Google Scholar

Ritanserin Related Antibodies

Top Publications Citing Use of Products

    Ritanserin purchased from MedChemExpress. Usage Cited in: Thorac Cancer. 2023 Mar 25.  [Abstract]

    Ritanserin (10 mg/mice; injecte; single daily for 15 days) significantly slows the growth of xenograft tumors (xenografts formed from A549 cells) in mice.

    View All 5-HT Receptor Isoform Specific Products:

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    5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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    Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

    View All Adrenergic Receptor Isoform Specific Products:

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    α adrenergic receptor β adrenergic receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors[1].

    IC50 & Target[1]

    5-HT2 Receptor

    0.9 nM (IC50)

    H1 Receptor

    35 nM (IC50)

    D2 Receptor

    70 nM (IC50)

    Adrenergic α1

    97 nM (IC50)

    Adrenergic α2

    150 nM (IC50)

    In Vitro

    Ritanserin (R 55667) is a highly potent, relatively selective, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine-H1 (IC50, 35 nM), Dopamine-D2 (IC50, 70 nM), Adrenergic-α1 (IC50, 97 nM), Adrenergic-α2 receptor (IC50, 150 nM)[1].

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

    Ritanserin Related Antibodies
    Clinical Trial
    Molecular Weight

    477.57

    Formula

    C27H25F2N3OS
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC1=C(C(N(C=CS2)C2=N1)=O)CCN(CC/3)CCC3=C(C4=CC=C(F)C=C4)\C5=CC=C(F)C=C5
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (52.35 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 2.0939 mL 10.4697 mL 20.9393 mL
    5 mM 0.4188 mL 2.0939 mL 4.1879 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 (stored under nitrogen). 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)

    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: ≥ 2.5 mg/mL (5.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    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: 99.78%

    COA (248 KB) HNMR (266 KB) LCMS (94 KB) Elemental Analysis Report (106 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month (stored under nitrogen). 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 2.0939 mL 10.4697 mL 20.9393 mL 52.3483 mL
    5 mM 0.4188 mL 2.0939 mL 4.1879 mL 10.4697 mL
    10 mM 0.2094 mL 1.0470 mL 2.0939 mL 5.2348 mL
    15 mM 0.1396 mL 0.6980 mL 1.3960 mL 3.4899 mL
    20 mM 0.1047 mL 0.5235 mL 1.0470 mL 2.6174 mL
    25 mM 0.0838 mL 0.4188 mL 0.8376 mL 2.0939 mL
    30 mM 0.0698 mL 0.3490 mL 0.6980 mL 1.7449 mL
    40 mM 0.0523 mL 0.2617 mL 0.5235 mL 1.3087 mL
    50 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0470 mL
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    Ritanserin 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:

    Ritanserin87051-43-2R 55667R55667R-556675-HT ReceptorHistamine ReceptorDopamine ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorInhibitorinhibitorinhibit

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