2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. AMG9810

AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.

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

CAS No. : 545395-94-6

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of AMG9810:

AMG9810 Related Antibodies

Top Publications Citing Use of Products

    AMG9810 purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 May 10;8(1):724.  [Abstract]

    AMG9810 (30 mg/kg; 200 μL; intraplantarly injected) attenuated IL-33-induced mechanical (E) and thermal hypersensitivity in ST2−/− mice.

    AMG9810 purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 May 31;39(10):e70657.  [Abstract]

    qPCR analysis of pro-inflammatory cytokines treated with TRPV1 in-hibitor. Levels of IL- 6 and C3 were measured in the primary astrocytes treated with Ctrl, 0.1 μg/mL LPS, 0.1 μg/mL LPS + 10 μM CZP, 0.1 μg/mL LPS + 30 μM CZP, 0.1 μg/mL LPS + 5 μM SB366791, 0.1 μg/mL LPS + 10 μM SB366791, 0.1 μg/mL LPS + 10 μM AMG9810 or 0.1 μg/mL LPS + 50 μM AMG9810.

    AMG9810 purchased from MedChemExpress. Usage Cited in: Neuron. 2024 Jun 5;112(11):1815-1831.e4.  [Abstract]

    AMG9810 (4 mg/kg; ip) markedly increased CBT in Trpv1+/+ mice, and the effect was absent in Trpv1-/- mice.

    AMG9810 purchased from MedChemExpress. Usage Cited in: Neuron. 2024 Jun 5;112(11):1815-1831.e4.  [Abstract]

    AMG9810 (4 mg/kg; ip) markedly increased CBT in Trpv1T634A/T634A mice.

    AMG9810 purchased from MedChemExpress. Usage Cited in: Stem Cell Rev Rep. 2021 Jun;17(3):999-1013.  [Abstract]

    AMG9810 (5 µM; 10 min) significantly decreased calcium flux response induced by capsaicin; withdrawal of Trpv1 antagonist AMG9810 led to rapid calcium transients in response to capsaicin in Dorsal root ganglia (DRG) derived satellite glial cells (SGCs).

    AMG9810 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2021 Jul;297(1):100806.  [Abstract]

    AMG9810 (10, 30 mg/kg; ip) significantly increased the thermal paw withdrawal latency compared with the control group in rats.

    View All TRP Channel Isoform Specific Products:

    View All Isoforms
    TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.

    IC50 & Target

    IC50: 24.5 nM (human TRPV1), 85.6 nM (rat TRPV1)[1]
    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    > 4 μM
    Compound: 9
    Agonist activity at TRPV1 expressed in CHO cells
    Agonist activity at TRPV1 expressed in CHO cells
    		[PMID: 17585749]
    CHO IC50
    0.023 x 10-6 M
    Compound: 1
    Inhibition of rat human chimera TRPV1 channel expressed in CHO cells
    Inhibition of rat human chimera TRPV1 channel expressed in CHO cells
    		[PMID: 17948977]
    CHO IC50
    0.136 x 10-6 M
    Compound: 91
    Inhibition of rat human chimera TRPV1 channel expressed in CHO cells
    Inhibition of rat human chimera TRPV1 channel expressed in CHO cells
    		[PMID: 17948977]
    CHO IC50
    1200 nM
    Compound: 34
    Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    		[PMID: 15634002]
    CHO IC50
    150 nM
    Compound: 1
    Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    		[PMID: 15634002]
    CHO IC50
    17 nM
    Compound: 1
    Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    		[PMID: 15634002]
    CHO IC50
    25 nM
    Compound: 6
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    CHO IC50
    294 nM
    Compound: 6
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    CHO IC50
    3200 nM
    Compound: 34
    Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    		[PMID: 15634002]
    CHO IC50
    350 nM
    Compound: 9
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx
    		[PMID: 17585749]
    CHO IC50
    79 nM
    Compound: 9
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx
    		[PMID: 17585749]
    CHO IC50
    86 nM
    Compound: 6
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    CHO IC50
    93 nM
    Compound: 6
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    Caco-2 CC50
    14.22 μM
    Compound: AMG-9810
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    		10.21203/rs.3.rs-23951/v1
    Caco-2 IC50
    14.97 μM
    Compound: AMG-9810
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    		10.21203/rs.3.rs-23951/v1
    In Vitro

    AMG9810 is a competitive antagonist of capsaicin activation (IC50 value for human TRPV1, 24.5±15.7 nM; rat TRPV1, 85.6±39.4 nM) and blocks all known modes of TRPV1 activation, including protons (IC50 value for rat TRPV1, 294±192 nM; human TRPV1, 92.7±72.8 nM), heat (IC50 value for rat TRPV1, 21±17 nM; human TRPV1, 15.8±10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. AMG9810 inhibits capsaicin-, proton-, heat-, and endogenous ligand-induced uptake of 45Ca2+ into TRPV1-expressing cells[1].

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

    AMG9810 Related Antibodies
    In Vivo

    AMG9810 is effective at preventing capsaicin-induced eye wiping in a dose-dependent manner, and it reverses thermal and mechanical hyperalgesia in a model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant. At effective doses, AMG9810 does not show any significant effects on motor function. AMG9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain[1]. AMG9810, promotes mouse skin tumor development. The topical application of AMG9810 results in a significant increase in the expression level of the epidermal growth factor receptor (EGFR) and its downstream Akt/mammalian target of rapamycin (mTOR)-signaling pathway[2].

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

    337.41

    Formula

    C21H23NO3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(NC1=CC=C(OCCO2)C2=C1)/C=C/C3=CC=C(C(C)(C)C)C=C3
    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 : ≥ 33 mg/mL (97.80 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 2.9638 mL 14.8188 mL 29.6375 mL
    5 mM 0.5928 mL 2.9638 mL 5.9275 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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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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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 (7.41 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 (7.41 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 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

    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).
    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: 99.48%

    SDS (392 KB)

    COA (245 KB) HNMR (269 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Cultured adult rat dorsal root ganglia neurons in 96-well plates are washed twice with release buffer to initiate the assay. CGRP release is induced by incubation of neurons with capsaicin for 10 min at room temperature. The cultures are preincubated with increasing concentrations of capsazepine or AMG9810 for 15 min, followed by 300 nM capsaicin activation for 10 min at room temperature. The extracellular medium is collected and the CGRP content is determined using a commercially kit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    To assess cyotoxicity of AMG9810, N/TERT1 cells are treated with different concentrations of AMG9810 (0.25, 0.5, 1, 5 μM) and cultured for various periods of time (24, 48, 72 h). The CellTiter 96 AQueous One Solution is added to each well and then cells are kept in a 37°C, 5% CO2 incubator for 1 h. Absorbance is then measured at 492 and 690 nm with a plate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Rats: AMG9810 is dissolved in DMSO. Rats are acclimated for 30 to 45 min in a 30×30×30-cm Plexiglas chambers before the intraperitoneal injection of either vehicle (DMSO) or AMG 9810. Injections are made over a 5-s period in the lower right ventral quadrant of the abdomen either 15, 30, or 60 min before intraocular application of capsaicin. Intraocular application of capsaicin (3 μg/20 μL in 10% ethanol/PBS) or vehicle (20 μL in 10% ethanol/PBS) is done with a pipette, and the number of front paw eye wipes is counted over a 5-min period in 1-min intervals [1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 2.9638 mL 14.8188 mL 29.6375 mL 74.0938 mL
    5 mM 0.5928 mL 2.9638 mL 5.9275 mL 14.8188 mL
    10 mM 0.2964 mL 1.4819 mL 2.9638 mL 7.4094 mL
    15 mM 0.1976 mL 0.9879 mL 1.9758 mL 4.9396 mL
    20 mM 0.1482 mL 0.7409 mL 1.4819 mL 3.7047 mL
    25 mM 0.1186 mL 0.5928 mL 1.1855 mL 2.9638 mL
    30 mM 0.0988 mL 0.4940 mL 0.9879 mL 2.4698 mL
    40 mM 0.0741 mL 0.3705 mL 0.7409 mL 1.8523 mL
    50 mM 0.0593 mL 0.2964 mL 0.5928 mL 1.4819 mL
    60 mM 0.0494 mL 0.2470 mL 0.4940 mL 1.2349 mL
    80 mM 0.0370 mL 0.1852 mL 0.3705 mL 0.9262 mL
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    AMG9810 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:

    AMG9810545395-94-6AMG 9810AMG-9810TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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