1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. SB-366791

SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation.

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

CAS No. : 472981-92-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SB-366791 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 15:e10102.  [Abstract]

    The 2:2 heterotetramer exhibited greatest capsaicin sensitivity (EC50 value of 2.24 × 10−5 mm\), reversibly inhibited by TRPV antagonist SB-366791 (0-100 μM).

    SB-366791 purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Sep 16;355(Pt A):120618.  [Abstract]

    The treatment with YPFND-H or SB-366791 (1 μM) mitigated the upregulation of TRPV1 by inhibiting p38 MAPK phosphorylation.

    SB-366791 purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Sep 16;355(Pt A):120618.  [Abstract]

    The treatment with YPFND-H or SB-366791 (1 μM) mitigated the upregulation of TRPV1 by inhibiting p38 MAPK phosphorylation.

    SB-366791 purchased from MedChemExpress. Usage Cited in: Neuron. 2024 Jun 5;112(11):1815-1831.e4.  [Abstract]

    Finally, SB366791 (3 μM) showed reduced inhibition of 2-APB-evoked currents of mTRPV1Y512W, mTRPV1S513A, mTRPV1S513T, mTRPV1L516F, mTRPV1T551S, mTRPV1T551C, and mTRPV1L670I, and the reduced potencies were confirmed using 9 μM SB366791 under conditions of channel activation by thermal stimulation.

    SB-366791 purchased from MedChemExpress. Usage Cited in: Dev Cell. 2024 Apr 1:S1534-5807(24)00180-1.  [Abstract]

    Dual inhibition of TRPV1 and PKD2 with SB-366791 (3 μM, 1h) and PKD2 knockdown further reduced force-induced Ca2+ release than inhibiting either alone. This result was corroborated by dual inhibition through TRPV1 knockdown and PKD2 knockdown, showing that TRPV1 and PKD2 contributed to the force-induced ER Ca2+ release in a cumulative manner.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation[1][2].

    IC50 & Target[2]

    hTRPV1

    5.7 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    0.27 μM
    Compound: SB-366791
    Antagonist activity at recombinant human TRPV1 channel expressed in CHO cells assessed as inhibition of capsiacin-induced Ca2+ flux by Fluo-3 dye based FLIPR assay
    Antagonist activity at recombinant human TRPV1 channel expressed in CHO cells assessed as inhibition of capsiacin-induced Ca2+ flux by Fluo-3 dye based FLIPR assay
    [PMID: 26850005]
    HEK293 IC50
    0.19 μM
    Compound: SB-366791
    Antagonist activity at recombinant human TRPV1 channel expressed in HEK293 cells assessed as inhibition of capsiacin-induced Ca2+ flux preincubated for 5 mins followed by capsiacin challenge by Fluo-4-AM dye based spectrofluorimetry
    Antagonist activity at recombinant human TRPV1 channel expressed in HEK293 cells assessed as inhibition of capsiacin-induced Ca2+ flux preincubated for 5 mins followed by capsiacin challenge by Fluo-4-AM dye based spectrofluorimetry
    [PMID: 26850005]
    In Vivo

    SB-366791 (30 μM) inhibits the frequency of miniature excitatory postsynaptic currents (EPSCs). SB-366791 (30 μM) reduces the frequency of spontaneous EPSCs in the spinal cord slices from FCA-treated rats. SB-366791(30 μM) inhibits the amplitude of C-fibre evoked EPSCs. SB-366791 has also been used in vivo to assess the potential analgesic action of the inhibition of TRPV1, and significantly inhibits capsaicin-induced hypothermia, eye wiping movements and vasodilatation in the knee joint. SB-366791 inhibits glutamatergic transmission via an apparently pre-synaptic mechanism(s)[1].

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

    Molecular Weight

    287.74

    Formula

    C16H14ClNO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC=CC(OC)=C1)/C=C/C2=CC=C(Cl)C=C2

    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
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (347.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4754 mL 17.3768 mL 34.7536 mL
    5 mM 0.6951 mL 3.4754 mL 6.9507 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, 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

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    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 (8.69 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (8.69 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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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    Dosing volume
    (per animal)

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    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).
    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
    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, 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
    DMSO 1 mM 3.4754 mL 17.3768 mL 34.7536 mL 86.8840 mL
    5 mM 0.6951 mL 3.4754 mL 6.9507 mL 17.3768 mL
    10 mM 0.3475 mL 1.7377 mL 3.4754 mL 8.6884 mL
    15 mM 0.2317 mL 1.1585 mL 2.3169 mL 5.7923 mL
    20 mM 0.1738 mL 0.8688 mL 1.7377 mL 4.3442 mL
    25 mM 0.1390 mL 0.6951 mL 1.3901 mL 3.4754 mL
    30 mM 0.1158 mL 0.5792 mL 1.1585 mL 2.8961 mL
    40 mM 0.0869 mL 0.4344 mL 0.8688 mL 2.1721 mL
    50 mM 0.0695 mL 0.3475 mL 0.6951 mL 1.7377 mL
    60 mM 0.0579 mL 0.2896 mL 0.5792 mL 1.4481 mL
    80 mM 0.0434 mL 0.2172 mL 0.4344 mL 1.0860 mL
    100 mM 0.0348 mL 0.1738 mL 0.3475 mL 0.8688 mL
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    • 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.

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    Product Name:
    SB-366791
    Cat. No.:
    HY-12245
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