2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. HC-030031

HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

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CAS 番号 : 349085-38-7

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カスタマーレビュー

Based on 37 publication(s) in Google Scholar

Other Forms of HC-030031:

HC-030031 関連抗体

Top Publications Citing Use of Products

顧客検証

In Vivo Efficacy Study
Cell Imaging/Staining
RT-PCR
Cell Proliferation/Viability Assay

    HC-030031 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jul 17:S2090-1232(25)00555-7.  [Abstract]

    TRPA1 mediates nepetalactone aversion via antennal sensilla. HC-030031 abolishes repellency.

    HC-030031 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jul 17:S2090-1232(25)00555-7.  [Abstract]

    Effect of HC030031 inhibitor on TRPA1 mRNA expression at 1 and 2 days, separately. HC030031 suppressed TRPA1 transcription in a dose-dependent pattern.

    HC-030031 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Aug 27;15(8):624.  [Abstract]

    TRPA1 inhibition suppressed osteoclast differentiation and function. TRAcP staining demonstrated that the quantity and area of positive cells were significantly reduced with HC-030031(10 μM).

    HC-030031 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2016 Sep 15;7:12840.  [Abstract]

    HC030031 (100 mg/kg; i.p.) significantly attenuated cold avoidance behavior enhanced by DMOG (400 mg/kg−1; i.p.; single dose) in mice.

    HC-030031 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2016 Sep 15;7:12840.  [Abstract]

    Compared with the vehicle-pre-administration group, pre-administration of DMOG (400 mg/kg) significantly increased the cold escape behaviour. The DMOG-enhanced cold escape behaviours were significantly attenuated by the TRPA1-selective antagonist HC030031 (HC) (100 mg/kg; 30 min before tests) or PBN (100 mg/kg).

    HC-030031 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2016 Mar 17;6:23261.  [Abstract]

    The TRPA1 antagonist HC-030031 (10, 30, and 50 mg/kg) or vehicle is administered i.p. immediately before initiating ischemia or in sham-treated mice.

    TRP Channel アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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    製品説明

    HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

    IC50 & Target

    TRPA1[1]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    18 μM
    Compound: HC030031
    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]
    HEK293 IC50
    4.9 μM
    Compound: 102
    Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of cinnamaldehyde-induced intracellular calcium influx by FLIPR
    Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of cinnamaldehyde-induced intracellular calcium influx by FLIPR
    		[PMID: 20356305]
    HEK293 IC50
    5.6 μM
    Compound: 3, HC-030031
    Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of BITC-induced increase in intracellular calcium concentration by Fluo4-AM based fluorometric assay
    Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of BITC-induced increase in intracellular calcium concentration by Fluo4-AM based fluorometric assay
    		[PMID: 22222037]
    HEK293 IC50
    6.2 μM
    Compound: 74, HC-030031
    Inhibition of human TRPA1 expressed in HEK293 cells after 10 mins by FLIPR assay
    Inhibition of human TRPA1 expressed in HEK293 cells after 10 mins by FLIPR assay
    		[PMID: 23121096]
    HEK293 IC50
    6.2 μM
    Compound: HC030031
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced increase in calcium influx by fluorescence analysis in presence of 5 uM AITC
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced increase in calcium influx by fluorescence analysis in presence of 5 uM AITC
    		[PMID: 30878828]
    HEK293 IC50
    7.5 μM
    Compound: 102
    Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular calcium influx by FLIPR
    Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular calcium influx by FLIPR
    		[PMID: 20356305]
    HEK293 IC50
    > 10 μM
    Compound: 3, HC-030031
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of 5H-dibenzo[b,e]azepine-10-carboxylic acid methyl ester-induced increase in intracellular calcium by Fluo4-AM based fluorometric assay
    Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of 5H-dibenzo[b,e]azepine-10-carboxylic acid methyl ester-induced increase in intracellular calcium by Fluo4-AM based fluorometric assay
    		[PMID: 22222037]
    IMR-90 IC50
    1.8 μM
    Compound: 1, HC-030031
    Antagonist activity at human TRPA1 expressed in human IMR90 cells assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis
    Antagonist activity at human TRPA1 expressed in human IMR90 cells assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis
    		[PMID: 22325155]
    体外実験

    HC-030031 reversibly blocks TRPA1 currents with a similar potency, regardless of the agonist used; this includes blockade of currents elicited by reversible agonists, such as AITC, or irreversible agonists, such as N-methyl maleimide. HC-030031 blocks activation of TRPA1 by N-methyl maleimide, which opens the channel irreversibly through cysteine modification. HC-030031 does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG, or NaV1.2 channels[1]. The potencies of HC-030031 versus cinnamaldehyde or allyl isothiocyanate (AITC or Mustard oil)-induced TRPA1 activation are 4.9±0.1 and 7.5±0.2 μM respectively (IC50). These findings are similar to the previously reported IC50 of 6.2 μM against AITC activation of TRPA1. The ability of HC-030031 to block TRPA1 activation is tested in a FLIPR calcium-influx assay using HEK-293 cells stably expressing human TRPA1. Concentrations of HC-030031 from 0.3 to 60 μM are incubated with cells for 10 minutes prior to addition of an EC60 concentration of either cinnamaldehyde or AITC. HC-030031 dose-dependently blocks cinnamaldehyde- and AITC-induced calcium influx with IC50 values of 4.9 and 7.5 μM, respectively[2].

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

    HC-030031 関連抗体
    体内実験

    After injection of AITC (50 μL of 10%) into the rat hind paw, HC-030031 (300 mg/kg) significantly reduces flinching during the first 5 min. Over the remainder of the hour, HC-030031 decreases flinch frequency, a result that mirrors the effects observed on formalin-induced flinching[1]. In the rat, oral administration of HC-030031 reduces AITC-induced nocifensive behaviors at a dose of 100 mg/kg. Moreover, oral HC-030031 (100 mg/kg) significantly reverses mechanical hypersensitivity in the more chronic models of Complete Freunds Adjuvant (CFA)-induced inflammatory pain and the spinal nerve ligation model of neuropathic pain. One hour post-oral administration, HC-030031 significantly reduces the lifting duration following 1% AITC injection (p<0.001)[2]. HC-030031 completely reverses the enhanced mechanical firing in inflamed mice (p<0.001)[3].

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

    355.39

    分子式

    C18H21N5O3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C2=C(N=CN2CC(NC3=CC=C(C(C)C)C=C3)=O)N(C)C(N1C)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 116.67 mg/mL (328.29 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 2.8138 mL 14.0691 mL 28.1381 mL
    5 mM 0.5628 mL 2.8138 mL 5.6276 mL
    10 mM 0.2814 mL 1.4069 mL 2.8138 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.

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    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:
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    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.85 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.85 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.

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    純度とドキュメンテーション

    純度: 99.65%

    COA (248 KB) HNMR (256 KB) RP-HPLC (232 KB) LCMS (327 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [2]

    HEK-293 cells stably expressing human TRPA1 are plated into 384-well plates at a density of 20,000 cells/well 24 hours prior to assaying. On the day of assay, cells are loaded with 4 μM Fluo-4 dye and 0.08% pluronic acid for 1 hour at room temperature in assay buffer consisting of Hank's balanced salt solution supplemented with 20 mM HEPES, 2.5 mM probenecid, and 4% TR-40. Calcium influx assays are performed using the Fluorometric Imaging Plate Reader (FLIPR) TETRA. Concentration-response curves are generated for the TRPA1 agonists cinnamaldehyde and AITC prior to antagonist testing so EC60 concentrations could be determined. Titrations of HC-030031 are made from a DMSO stock solution and DMSO is kept to a constant of 0.4% in the assay. The antagonist is incubated with the cells for 10 minutes before the addition of an EC60 concentration of either cinnamaldehyde (18 μM) or AITC (6 μM) and calcium influx is monitored for an additional 10 minutes[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [2][3]

    Rats[2]
    Male Sprague-Dawley rats (200-500 g) are used in all experiments. HC-030031 (100, 300 mg/kg) is used. For all experiments, HC-030031 is suspended in 0.5% Methylcellulose and the drug is dosed p.o. at a volume of 10 mL/kg. Naproxen (20 mg/kg) is dissolved in sterile water and dosed p.o. to serve as a positive comparator for the CFA experiment. Pregabalin (20 mg/kg) is dissolved in sterile water and dosed p.o. to serve as a positive comparator for the neuropathic pain experiment.
    Mice[3]
    Adult male C57BL/6 mice (8-12 weeks old) are used. Mice are injected with a 30 µL emulsion of undiluted CFA into the medial left plantar hind paw. The vehicle control group is injected with 30 µL of sterile 0.9% saline solution. Two days after injection, at the peak of hypersensitivity, the magnitude of inflammation is measured at the midpoint of the hind paw using digital calipers (VWR). For one experiment, the membrane-impermeable sodium channel inhibitor lidocaine N-ethyl-bromide, also known as QX-314, (0.2% in saline; 30 µL) is injected with or without the TRPA1 agonist cinnamaldehyde (30 µM) into the left plantar hind paw 2 days post CFA injection. For another experiment, the TRPA1 antagonist HC-030031 (100 µg in 30 µL of 0.5% DMSO and 0.25% Tween-80 in PBS) is injected into the left plantar hind paw 2 days post CFA injection. Vehicle controls are injected with 30 µL 0.5% DMSO and 0.25% Tween-80 in PBS. All behavioral assays are completed between 1 and 4 hours following the QX-314, HC-030031 or vehicle injections.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 2.8138 mL 14.0691 mL 28.1381 mL 70.3453 mL
    5 mM 0.5628 mL 2.8138 mL 5.6276 mL 14.0691 mL
    10 mM 0.2814 mL 1.4069 mL 2.8138 mL 7.0345 mL
    15 mM 0.1876 mL 0.9379 mL 1.8759 mL 4.6897 mL
    20 mM 0.1407 mL 0.7035 mL 1.4069 mL 3.5173 mL
    25 mM 0.1126 mL 0.5628 mL 1.1255 mL 2.8138 mL
    30 mM 0.0938 mL 0.4690 mL 0.9379 mL 2.3448 mL
    40 mM 0.0703 mL 0.3517 mL 0.7035 mL 1.7586 mL
    50 mM 0.0563 mL 0.2814 mL 0.5628 mL 1.4069 mL
    60 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1724 mL
    80 mM 0.0352 mL 0.1759 mL 0.3517 mL 0.8793 mL
    100 mM 0.0281 mL 0.1407 mL 0.2814 mL 0.7035 mL
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    HC-030031 Related Classifications

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    Keywords:

    HC-030031349085-38-7HC030031HC 030031TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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    製品名:
    HC-030031
    製品番号:
    HY-15064
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