2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. A-967079

A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the blood-brain barrier.

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

CAS No. : 1170613-55-4

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of A-967079:

A-967079 Related Antibodies

Top Publications Citing Use of Products

    A-967079 purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 Dec 1;9(1):19.  [Abstract]

    Whole-cell TRPA1 currents elicited by the application of 1 mM 4-A and 500 μM SH. This response was blocked by 10 μM A-967079 (A-96), a selective TRPA1 inhibitor.

    A-967079 purchased from MedChemExpress. Usage Cited in: Headache. 2025 Oct 24.  [Abstract]

    CGRP levels were measured in male and female dura mater following baseline collection and stimulation with the TRPA1 antagonist A-967079 (3 µM), TRPM3 agonist CIM0216 (100 µM), or their combination. In both sexes, CIM0216 increased CGRP release compared to baseline and vehicle.

    A-967079 purchased from MedChemExpress. Usage Cited in: Headache. 2025 Oct 24.  [Abstract]

    CGRP levels in male dura mater and male TG were measured at baseline and after stimulation with the TRPA1 antagonist A-967079 (3 µM), the TRPA1 agonist supercinnamaldehyde (100 µM), or their combination. Supercinnamaldehyde increased CGRP release in both dura mater and TG. This effect was reduced when tissues were pretreated with A-967079.

    A-967079 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2024 May 14.  [Abstract]

    Effect of A 967079 (1 μM), another structurally unrelated TRPA1 channel antagonist on the peak amplitude of Ca2+ traces evoked by AITC (30 μM) in control and inflammatory conditions, as indicated in the figure.

    A-967079 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2024 May 14.  [Abstract]

    Effect of poly(I:C), and TRPA1 channel agonists and antagonists on mitochondrial superoxide production in 60 min. The following treatments were applied, as indicated in the figure: 100 μM AITC (AITC), 300 μM cinnamaldehyde (CA), 10 μM HC-030031 (HC), and 1 μM A 967079 (A96) in the presence or absence of poly(I:C).

    A-967079 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2024 Jan 31;16(3):609.  [Abstract]

    PANC-1 and MIA PaCa-2 cells were pre-treated with the selective TRPA1 pore function inhibitor (A-967079) for 1 h and then left untreated or stimulated with FGF2 for 24 h. Western blot analysis showed that the inhibition of the TRPA1 pore function did not impact PANC-1 cell response to FGF2 in terms of E-cadherin/vimentin modulation toward EMT enhancement.

    A-967079 purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2024 Dec 13;10(12):4327-4336.  [Abstract]

    Chemical structure of A-967079 and the plaque assay images of A-967079 (0-10 μM) against EV-D68 US/MO/14-18947 in RD cells. The plaques were quantified using Image J. Images were representatives of two independent replicates.

    A-967079 purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2024 Dec 13;10(12):4327-4336.  [Abstract]

    Broad-spectrum antiviral activity of A-967079 in RD cells.

    A-967079 purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2024 Dec 13;10(12):4327-4336.  [Abstract]

    Plaque assay images of A-967079 (0-3 μM) against EV-D68 US/MO/14-18947 in A549 cells. The plaques were quantified using Image J. Images were representatives of two independent replicates.

    A-967079 purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2024 Dec 13;10(12):4327-4336.  [Abstract]

    A-967079 (0-3 μM) inhibited EV-D68 VP1 synthesis in immunofluorescence assay. RD cells were infected by EV-D68 US/MO/14-18947 at a MOI of 1. Cells were fixed 9 hours postinfection. Cells were stained with anti-VP1 and Hoechst to detect EV-D68 VP1 and nucleus. The images were representatives of three independent experiments.

    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

    A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the blood-brain barrier[1].

    IC50 & Target

    IC50: 67 nM (human TRPA1 receptor), 289 nM (rat TRPA1 receptor)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    79 nM
    Compound: A967079
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
    		[PMID: 30878828]
    In Vivo

    Systemic injection of A-967079 (30 μmol/kg, i.v.) decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation of the ipsilateral hind paw in uninjured and CFA-inflamed rats. Similar to its actions in uninjured rats, administration of A-967079 (30 μmol/kg, i.v.) to complete Freund's adjuvant (CFA)-inflamed rats significantly reduces WDR neuronal responses to noxious pinch stimulation compared to baseline firing (p=0.0013, repeated-measures ANOVA) and the vehicle group (p=0.0001, two-way ANOVA). The maximum observed effect (61.1±10.97% decrease from baseline levels) on pinch-evoked activity in inflamed rats occur 35 min after injection. In contrast to uninjured rats, injection of A-967079 to CFA-inflamed rats also significantly (p=0.0004, and p=0.0001 for the repeated-measures and two-way ANOVA's, respectively) reduces responses of WDR neurons to 10-g von Frey hair stimulation. The maximal observed decrease in von Frey-evoked activity is 67.69±18.39% from baseline levels (35 min post-injection), and is thus comparable to the effects of A-967079 on pinch-evoked activity in inflamed rats[1].

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

    207.24

    Formula

    C12H14FNO
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCC(/C(C)=C/C1=CC=C(F)C=C1)=N\O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (482.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.8253 mL 24.1266 mL 48.2532 mL
    5 mM 0.9651 mL 4.8253 mL 9.6506 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. 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)

    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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (12.06 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: ≥ 2.5 mg/mL (12.06 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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    mg/kg

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    (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 +
    % 
    +
    %
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    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: 99.30%

    SDS (251 KB)

    COA (245 KB) LCMS (88 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Rats[1]
    Male Sprague-Dawley rats (250-400 g) are used for all experiments and are housed in a temperature controlled room with a 12/12-hr day/night cycle. Food and water are available ad libitum. Spontaneous and evoked neuronal activity is then measured 5, 15, 25, and 35 min after systemic injection of A-967079 (30 μmol/kg, i.v.) or vehicle (polyethylene glycol). The intravenous injection of A-967079 or vehicle is completed over a 6-7 min period. The i.v. dose of A-967079 is selected based on extrapolated plasma levels that are effective in behavioral studies[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, 6 months; -20°C, 1 month. 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 4.8253 mL 24.1266 mL 48.2532 mL 120.6331 mL
    5 mM 0.9651 mL 4.8253 mL 9.6506 mL 24.1266 mL
    10 mM 0.4825 mL 2.4127 mL 4.8253 mL 12.0633 mL
    15 mM 0.3217 mL 1.6084 mL 3.2169 mL 8.0422 mL
    20 mM 0.2413 mL 1.2063 mL 2.4127 mL 6.0317 mL
    25 mM 0.1930 mL 0.9651 mL 1.9301 mL 4.8253 mL
    30 mM 0.1608 mL 0.8042 mL 1.6084 mL 4.0211 mL
    40 mM 0.1206 mL 0.6032 mL 1.2063 mL 3.0158 mL
    50 mM 0.0965 mL 0.4825 mL 0.9651 mL 2.4127 mL
    60 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0106 mL
    80 mM 0.0603 mL 0.3016 mL 0.6032 mL 1.5079 mL
    100 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2063 mL
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    A-967079 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:

    A-9670791170613-55-4A967079A 967079TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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