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  4. Capsaicin

Capsaicin  (Synonyms: (E)-Capsaicin)

Cat. No.: HY-10448 Purity: 99.85%
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Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain-relieving, antioxidant, anti-inflammatory, anti-cancer and certain neurotoxic effects.

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

Capsaicin Chemical Structure

Capsaicin Chemical Structure

CAS No. : 404-86-4

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Customer Review

Based on 43 publication(s) in Google Scholar

Other Forms of Capsaicin:

Top Publications Citing Use of Products

40 Publications Citing Use of MCE Capsaicin

WB
Cell Viability Assay

    Capsaicin purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jun 24;10(17):7906-7920.  [Abstract]

    CNE2 and SUNE1 cell growth is inhibited by Capsaicin in a dose-dependent manner.

    Capsaicin purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jun 24;10(17):7906-7920.  [Abstract]

    The expression of cell cycle-associated molecules is altered by Capsaicin treatment in both cell lines.The cell-cycle inhibitor p27Kip1 is upregulated after Capsaicin treatment while the G1-S phase transition marker cyclin D1 is downregulated. p38 phosphorylation levels are also decreased following capsaicin treatment.

    Capsaicin purchased from MedChemExpress. Usage Cited in: Clin Exp Pharmacol Physiol. 2017 Jul;44(7):803-814.  [Abstract]

    Western blot analysis showing that the CAP (0.5 mg/kg) injection inhibits the increase of p65 expression and phosphorylation at 24 h after I/R injury.

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    Description

    Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain-relieving, antioxidant, anti-inflammatory, anti-cancer and certain neurotoxic effects[1][2].

    IC50 & Target

    EC50: 290 nM (hTRPV1, in HEK293 cell)[1]

    Cellular Effect
    Cell Line Type Value Description References
    A2058 IC50
    > 100 μM
    Compound: Capsaicin
    Cytotoxicity against human A2058 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human A2058 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    [PMID: 31104785]
    B16-F10 IC50
    > 100 μM
    Compound: Capsaicin
    Cytotoxicity against mouse B16F10 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against mouse B16F10 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    [PMID: 31104785]
    BGC-823 IC50
    4.659 μM
    Compound: 1
    Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability incubated for 5 days by MTS assay
    Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability incubated for 5 days by MTS assay
    [PMID: 33581557]
    CHO EC50
    25.9 nM
    Compound: 1; CAP
    Agonist activity at human TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
    Agonist activity at human TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
    [PMID: 31702924]
    CHO EC50
    44.8 nM
    Compound: 1; CAP
    Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
    Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method
    [PMID: 31702924]
    CHO EC50
    44.8 nM
    Compound: Capsaicin
    In vitro [Ca2+] influx relative to capsaicin by Rat Vanilloid receptor (VR1) expressing CHO cells
    In vitro [Ca2+] influx relative to capsaicin by Rat Vanilloid receptor (VR1) expressing CHO cells
    [PMID: 12825950]
    HBMEC-2 EC50
    16.37 μM
    Compound: Capsaicin
    Neuroprotective activity against H2O2-induced cell damage in human HBMEC2 cells assessed as increase in cell viability preincubated for 24 hrs followed by H2O2 addition and measured after 4 hrs by MTT assay
    Neuroprotective activity against H2O2-induced cell damage in human HBMEC2 cells assessed as increase in cell viability preincubated for 24 hrs followed by H2O2 addition and measured after 4 hrs by MTT assay
    [PMID: 31541868]
    HCT-116 IC50
    40.16 μM
    Compound: Capsaicin
    Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by crystal violet staining based assay
    Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by crystal violet staining based assay
    [PMID: 34795858]
    HEK293 EC50
    0.0039 μM
    Compound: Capsaicin
    Agonist activity at human TRPV1 ion channel expressed in HEK293 cells assessed as calcium influx by fluo-4-Am-based fluorimetry
    Agonist activity at human TRPV1 ion channel expressed in HEK293 cells assessed as calcium influx by fluo-4-Am-based fluorimetry
    [PMID: 22257892]
    HEK293 EC50
    0.0053 μM
    Compound: 1a
    Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as Ca2+ influx by Fluo-4 dye based assay
    Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as Ca2+ influx by Fluo-4 dye based assay
    [PMID: 25666822]
    HEK293 IC50
    0.008 μM
    Compound: 1a
    Antagonist activity against human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx pre-treated 5 mins before capsaicin addition by Fluo-4 dye based assay
    Antagonist activity against human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx pre-treated 5 mins before capsaicin addition by Fluo-4 dye based assay
    [PMID: 25666822]
    HeLa IC50
    > 50 μM
    Compound: CAP
    Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
    Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
    [PMID: 29685681]
    K562 IC50
    49.41 μM
    Compound: CAP
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    [PMID: 29685681]
    MCF7 IC50
    100 μM
    Compound: Capsaicin
    Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition by MTT assay
    Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition by MTT assay
    [PMID: 33508189]
    MCF7 IC50
    49.97 μM
    Compound: CAP
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 29685681]
    MDA-MB-231 IC50
    120 μM
    Compound: 24
    Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
    [PMID: 32686940]
    NCI-H460 IC50
    30.66 μM
    Compound: Capsaicin
    Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition measured after 72 hrs by crystal violet staining based assay
    Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition measured after 72 hrs by crystal violet staining based assay
    [PMID: 34795858]
    SH-SY5Y EC50
    14.02 μM
    Compound: Capsaicin
    Neuroprotective activity against H2O2-induced cell damage in human SH-SY5Y cells assessed as increase in cell viability preincubated for 24 hrs followed by H2O2 addition and measured after 4 hrs by MTT assay
    Neuroprotective activity against H2O2-induced cell damage in human SH-SY5Y cells assessed as increase in cell viability preincubated for 24 hrs followed by H2O2 addition and measured after 4 hrs by MTT assay
    [PMID: 31541868]
    SH-SY5Y EC50
    2.32 μM
    Compound: Capsaicin
    Agonist activity at rat TRPV1 expressed in human SH-SY5Y cells assessed as intracellular calcium accumulation by Fluo-4 NW dye based fluorescence assay
    Agonist activity at rat TRPV1 expressed in human SH-SY5Y cells assessed as intracellular calcium accumulation by Fluo-4 NW dye based fluorescence assay
    [PMID: 30783490]
    SK-MEL-25 IC50
    > 100 μM
    Compound: Capsaicin
    Cytotoxicity against human SK-MEL-25 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human SK-MEL-25 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    [PMID: 31104785]
    SK-OV-3 IC50
    22.03 μM
    Compound: Capsaicin
    Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by crystal violet staining based assay
    Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by crystal violet staining based assay
    [PMID: 34795858]
    T47D IC50
    100 μM
    Compound: Capsaicin
    Antiproliferative activity in human T47D cells assessed as cell growth inhibition by MTT assay
    Antiproliferative activity in human T47D cells assessed as cell growth inhibition by MTT assay
    [PMID: 33508189]
    U-87MG ATCC IC50
    > 100 μM
    Compound: Capsaicin
    Cytotoxicity against human U87 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human U87 cells assessed as decrease in cell viability incubated for 24 hrs by MTT assay
    [PMID: 31104785]
    In Vitro

    Capsaicin (50-300 μM; 24-72 hours) shows an augmented decrease in cell growth in a dose- and time-dependent manner. The observed IC50 value is around 150 μM[2].
    Capsaicin (50-300 μM; 24-72 hours) shows increase in cytosolic cytochrome c, activation of caspase 3 and PARP (p85) levels, and decreases anti-apoptotic Bcl-2 protein and increases pro-apoptotic Bad/Bax expression[2].
    Capsaicin increases the nuclear condensation, nuclear DNA fragmentation and sub-G1 DNA content[2].
    Capsaicin suppresses the cell cycle progression at the G1/S phase in FaDu cells by decreasing the expression of the regulators of cyclin B1 and D1, as well as cyclin-dependent protein kinases cdk-1, cdk-2 and cdk-4[2].

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

    Cell Viability Assay[2]

    Cell Line: Human pharyngeal squamous carcinoma cells (FaDu) cells
    Concentration: 50 µM, 100 µM, 200 µM, and 300 µM
    Incubation Time: 24 hours, 48 hours and 72 hours
    Result: Showed an augmented decrease in cell growth.

    Apoptosis Analysis[2]

    Cell Line: FaDu cells
    Concentration: 50 µM, 100 µM and 200 µM
    Incubation Time: 12 hours
    Result: Increased the activity of caspase 3 in a time-dependent manner.

    Western Blot Analysis[2]

    Cell Line: FaDu cells
    Concentration: 200 µM
    Incubation Time: 24 hours
    Result: The observed activation of caspase 3 and PARP (p85) levels.
    In Vivo

    Capsaicin suppresses the development of lung carcinoma by amending the protein expressions of apoptotic regulators p53, Bcl-2, Bax and caspase-3[2].
    Capsaicin (2 μg in 40 μL per mice, injected into the plantar surface of the left hind paw) induces pain-related behaviour in mice[4].
    Capsaicin (3-30 μg in 10 μL per rat, plantar injection) induces secondary mechanical hypersensitivity (SMH) (used clinically as a model to potentially predict neuropathic pain) in rats[5].
    Capsaicin (0-500 μg in 25 μL per rat, injected subcutaneously into the center of the right vibrissae pad) induces pain in the orofacial region or rats[6].
    In high dose, Capsaicin may should be adminstered under anesthesia condition[7][8].
    Capsaicin is more pungent than Dihydrocapsaicin (HY-N0361) [9].
    Note: The spicy taste is choking, please take precautions.

    Capsaicin ((E)-Capsaicin) LD50 under different circumstances:

    Animal Backgroud Route LD50 References
    Rat adult ip 10 mg/kg [10]
    female; 51-54 g ip 10.40-13.20 mg/kg [11]
    female; 141 g ip 9.50 mg/kg [11]
    male po 161.2 mg/kg [12]
    female po 148.1 mg/kg [12]
    Mice male; 25-35 g iv 0.56 mg/kg [11]
    male po 118.8 mg/kg [12]
    male ip 7.56 mg/kg [10]
    female po 97.4 mg/kg [12]
    female; 30 g ip 6.50 mg/kg [11]
    ip 7.65 mg/kg [11]
    im 7.80 mg/kg [11]
    sc 9.00 mg/kg [11]
    po 60-75 mg/kg [11]
    po 190 mg/kg [11]
    pr >218 mg/kg [11]
    dermal >512 mg/kg [11]
    intratracheal 1.60 mg/kg [11]
    Hamster male; 65 g ip >120 mg/kg [11]
    Guinea Pig male; 405 g ip >1.10 mg/kg [11]
    Rabbit adult; 503 g ip >50 mg/kg [11]

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

    Animal Model: Swiss albino mice (20-25 g; 8-10 weeks old) induced by Benzo(a)pyrene[3]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal administration; once in a week; for 14 weeks
    Result: Inhibited the development of mice lung carcinogenesis.
    Clinical Trial
    Molecular Weight

    305.41

    Formula

    C18H27NO3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)/C=C/CCCCC(NCC1=CC=C(O)C(OC)=C1)=O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (327.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 100 mg/mL (327.43 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2743 mL 16.3714 mL 32.7429 mL
    5 mM 0.6549 mL 3.2743 mL 6.5486 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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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    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% EtOH    90% Corn Oil

      Solubility: ≥ 20 mg/mL (65.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 20 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 EtOH stock solution (200.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (8.19 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.
    In Vivo Dissolution Calculator
    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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    %
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    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, 1 year; -20°C, 6 months (protect from light)

    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: 99.85%

    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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 3.2743 mL 16.3714 mL 32.7429 mL 81.8572 mL
    5 mM 0.6549 mL 3.2743 mL 6.5486 mL 16.3714 mL
    10 mM 0.3274 mL 1.6371 mL 3.2743 mL 8.1857 mL
    15 mM 0.2183 mL 1.0914 mL 2.1829 mL 5.4571 mL
    20 mM 0.1637 mL 0.8186 mL 1.6371 mL 4.0929 mL
    25 mM 0.1310 mL 0.6549 mL 1.3097 mL 3.2743 mL
    30 mM 0.1091 mL 0.5457 mL 1.0914 mL 2.7286 mL
    40 mM 0.0819 mL 0.4093 mL 0.8186 mL 2.0464 mL
    50 mM 0.0655 mL 0.3274 mL 0.6549 mL 1.6371 mL
    60 mM 0.0546 mL 0.2729 mL 0.5457 mL 1.3643 mL
    80 mM 0.0409 mL 0.2046 mL 0.4093 mL 1.0232 mL
    100 mM 0.0327 mL 0.1637 mL 0.3274 mL 0.8186 mL
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