製品番号: HY-15064

HC-030031

Name: HC-030031
Brand: MedChemExpress
SKU: HY-15064
Price: 35.00 USD
Availability: InStock
Rating: 5 (37 reviews)

37 Cited Publications

カスタマーレビュー

Based on 37 publication(s) in Google Scholar

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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純度 : 99.65%
CAS 番号: 349085-38-7
分子式: C₁₈H₂₁N₅O₃
分子量:355.39

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

HC-030031 構造式

CAS 番号: 349085-38-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (37)
溶剤 & 溶解度
- 体外
- 体内
プロトコル (1)
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

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]

TRP Channel アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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. Further protocols information, click here.

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.

化学情報

CAS 番号 349085-38-7
性状 Solid
分子量 355.39
分子式 C₁₈H₂₁N₅O₃
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

Publications (37)

All In Vivo Efficacy StudyCell Imaging/StainingRT-PCRCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Commun

Cold sensitivity of TRPA1 is unveiled by the prolyl hydroxylation blockade-induced sensitization to ROS. [Abstract]

2016 Sep 15:7:12840. PMID: 27628562

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).
J Adv Res

TRPA1-kinase axis polarization: Nepetalactone drives pest repulsion and predator attraction via divergent PKC/CaMKII signaling. [Abstract]

2025 Jul 17:S2090-1232(25)00555-7. PMID: 40683383

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.
Cell Death Dis

TRPA1 promotes overactive bladder progression by activating the NLRP3 inflammasome and driving pyroptosis. [Abstract]

2026 Feb 16;17(1):226. PMID: 41698890
Cell Death Dis

TRPA1 aggravates osteoclastogenesis and osteoporosis through activating endoplasmic reticulum stress mediated by SRXN1. [Abstract]

2024 Aug 27;15(8):624. PMID: 39191723

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).
Int J Nanomedicine

Os Draconis-Derived Nanoparticles Improve Insomnia Symptoms by Activating Calcium-Dependent 5-HT Release and the Vagal-NTS Pathway. [Abstract]

2025 Dec 2:20:14329-14341. PMID: 41368289
Clin Transl Med

Dissecting the effect of ileal faecal diversion on the intestine using single-cell sequencing. [Abstract]

2023 Jul;13(7):e1321. PMID: 37400975
ACS Appl Mater Interfaces

Enhancing Photodynamic Therapy Efficacy via Photo-Triggered Calcium Overload and Oxygen Delivery in Tumor Hypoxia Management. [Abstract]

2025 Feb 5;17(5):8403-8416. PMID: 39853325
Cell Rep

Mechanosensitive calcium channels and integrins coordinate the reprogramming of colorectal cancer cells into a fetal-like state. [Abstract]

2025 Sep 22;44(10):116308. PMID: 40986425
J Ethnopharmacol

Artemisia argyi volatile oil ameliorates allergic contact dermatitis via modulating TRPA1/CGRP signaling. [Abstract]

2024 Nov 15:334:118580. PMID: 39019419
J Ethnopharmacol

TRPA1 is involved in the inhibitory effect of Ke-teng-zi on allergic contact dermatitis via MAPK and JAK/STAT3 signaling pathways. [Abstract]

2023 May 10:307:116182. PMID: 36706935
Cell Mol Life Sci

Role of transient receptor potential ankyrin 1 in idiopathic pulmonary fibrosis: modulation of M2 macrophage polarization. [Abstract]

2024 Apr 18;81(1):187. PMID: 38635081
Eur J Pharmacol

Mechanisms of the PD-1/PD-L1 pathway in itch: From acute itch model establishment to the role in chronic itch in mouse. [Abstract]

2023 Dec 5:960:176128. PMID: 37866747
Int J Mol Sci

TRPA1-Activated Peptides from Saiga Antelope Horn: Screening, Interaction Mechanism, and Bioactivity. [Abstract]

2025 Feb 27;26(5):2119. PMID: 40076741
Biomolecules

PAR2 Participates in the Development of Cough Hypersensitivity in Guinea Pigs by Regulating TRPA1 Through PKC. [Abstract]

2025 Feb 1;15(2):208. PMID: 40001511
Front Pharmacol

Desensitization of TRPA1 by dimethyl itaconate attenuates acute and chronic pain in mice. [Abstract]

2025 Sep 29:16:1671461. PMID: 41089843
Toxicology

Elevated intracellular Ca2+ functions downstream of mitodysfunction to induce Wallerian-like degeneration and necroptosis in organophosphorus-induced delayed neuropathy. [Abstract]

2024 May:504:153812. PMID: 38653376
J Neuroendocrinol

The caudal neurosecretory system: A novel thermosensitive tissue and its signal pathway in olive flounder (Paralichthys olivaceus). [Abstract]

2020 Jun;32(6):e12876. PMID: 32542811
Sci Rep

Hypoxia-induced sensitisation of TRPA1 in painful dysesthesia evoked by transient hindlimb ischemia/reperfusion in mice. [Abstract]

2016 Mar 17:6:23261. PMID: 26983498

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.
Neuropharmacology

Deficiency of KIF15 contributes to oxaliplatin-induced cold hypersensitivity by limiting annexin A2 and enhancing TRPA1 localization in DRG neuronal membrane. [Abstract]

2025 May 15:269:110343. PMID: 39914618
J Inflamm Res

Neural-Inflammation Mechanism of Spinal Palmitic Acid Promoting Atopic Dermatitis in Mice. [Abstract]

2025 Jun 17:18:7907-7919. PMID: 40546406
Environ Toxicol Pharmacol

Exposure to formaldehyde at low temperatures aggravates allergic asthma involved in transient receptor potential ion channel. [Abstract]

2020 Nov:80:103469. PMID: 32798733
iScience

T cell death-associated gene 8-mediated distinct signaling pathways modulate the early and late phases of neuropathic pain. [Abstract]

2024 Sep 13;27(10):110955. PMID: 39381739
Aquaculture

2023 Dec 15, 577, 739927.
Aquaculture

2021, 736537.
J Endod

Activation of Transient Receptor Potential Ankyrin 1 and Vanilloid 1 Channels Promotes Odontogenic Differentiation of Human Dental Pulp Cells. [Abstract]

2021 Sep;47(9):1409-1416. PMID: 34126160
Mol Pain

Histamine H4 receptor and TRPV1 mediate itch induced by cadaverine, a metabolite of the microbiome. [Abstract]

2024 Jan-Dec:20:17448069241272149. PMID: 39079948
Mol Pain

X-ray induces mechanical and heat allodynia in mouse via TRPA1 and TRPV1 activation. [Abstract]

2019 Jan-Dec:15:1744806919849201. PMID: 31012378
Cell Immunol

TRPV4 is not the molecular sensor for bacterial lipopolysaccharides-induced calcium signaling. [Abstract]

2023 Jan:383:104651. PMID: 36493524
Neuroscience

Inhibition of TRPA1 Attenuates Oxidative Stress-induced Damage After Traumatic Brain Injury via the ERK/AKT Signaling Pathway. [Abstract]

2022 Jul 1:494:51-68. PMID: 35158017
Biol Reprod

Aerobic exercises regulate the epididymal anion homeostasis of high-fat diet induced obese rats through TRPA1-mediated cl- and HCO3- secretion. [Abstract]

2023 Jul 11;109(1):53-64. PMID: 37154585
Toxicol Lett

Co-exposure to polystyrene microplastics and di-(2-ethylhexyl) phthalate aggravates allergic asthma through the TRPA1-p38 MAPK pathway. [Abstract]

2023 Aug 1:384:73-85. PMID: 37500026
Am J Physiol Regul Integr Comp Physiol

TRPA1 channels modulate cutaneous vasodilation during exercise in the heat in young adults when NOS is inhibited. [Abstract]

2025 Feb 10. PMID: 39925087
J Nat Med

Huanglian decoction prevents and treats radiation-induced intestinal injury in lung cancer by regulating endoplasmic reticulum stress. [Abstract]

2025 Jan;79(1):143-161. PMID: 39636341
Cryobiology

Effects of spray cryotherapy on cough receptors and airway microenvironment in a canine model of chronic bronchitis. [Abstract]

2023 Dec:113:104569. PMID: 37597598
J Mol Histol

Functional expression of TRPA1 channel, TRPV1 channel and TMEM100 in human odontoblasts. [Abstract]

2021 Oct;52(5):1105-1114. PMID: 34514518
Transl Pediatr

Chenodeoxycholic acid activates the TGR5/TRPA1-5-HT pathway to regulate intestinal motility in breastfed infants and mouse models. [Abstract]

2025 Jun 27;14(6):1213-1229. PMID: 40688229
Kyoto University

2017 Mar.

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)

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Stock Solution Working Solution

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 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.

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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Working solution concentration: 0.22 mg/mL

プロトコル

All Cell Biology

Ca²⁺ Staining Technique
Ca²⁺ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca²⁺ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.

純度とドキュメンテーション

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純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[1]. McNamara CR, et al. TRPA1 mediates formalin-induced pain. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30. [Content Brief]

[2]. Eid SR, et al. HC-030031, a TRPA1 selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity. Mol Pain. 2008 Oct 27;4:48. [Content Brief]

[3]. Lennertz RC, et al. TRPA1 mediates mechanical sensitization in nociceptors during inflammation. PLoS One. 2012;7(8):e43597. [Content Brief]

[4]. Miyake T, et al. Cold sensitivity of TRPA1 is unveiled by the prolyl hydroxylation blockade-induced sensitization to ROS. Nat Commun. 2016 Sep 15;7:12840. [Content Brief]

[5]. So K, et al. Hypoxia-induced sensitisation of TRPA1 in painful dysesthesia evoked by transient hindlimb ischemia/reperfusion in mice. Sci Rep. 2016 Mar 17;6:23261. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

37 Cited Publications

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HC-030031

MedChemExpress（MCE）の使用を引用している文献 HC-030031

TRP Channel アイソフォーム固有の製品をすべて表示

生物活性