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AB120554

HC-030031, TRPA1 blocker

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(8 Publications)

MW 355.4 Da, Purity >99%. Selective TRPA1 blocker, orally active. Blocks TRPA1-mediated currents (IC50 = 0.7 μM) and selective over TRPV1, TRPV3, TRPV4, hERG, and NaV1.2 channels (IC50 >10 μM). Does not display any significant binding to 41 other receptors, ion channels, and transporters nor functional modulation of 7 enzymes that are known to modulate pain signaling.

View Alternative Names

ANKTM 1, Ankyrin-like with transmembrane domains protein 1, TRPA1_HUMAN, Transformation-sensitive protein p120, Transient receptor potential cation channel subfamily A member 1

1 Images
Chemical Structure - HC-030031, TRPA1 blocker (AB120554)
  • Chemical Structure

Lab

Chemical Structure - HC-030031, TRPA1 blocker (AB120554)

2D chemical structure image of ab120554, HC-030031, TRPA1 blocker

Key facts

CAS number

349085-38-7

Purity

>99%

Form

Solid

form

Molecular weight

355.4 Da

Molecular formula

C<sub>1</sub><sub>8</sub>H<sub>2</sub><sub>1</sub>N<sub>5</sub>O<sub>3</sub>

PubChem

1150897

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Biochemical name

2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(4-isopropylphenyl)acetamide

Biological description

Selective TRPA1 blocker, orally active. Blocks TRPA1-mediated currents (IC50 = 0.7 μM) and selective over TRPV1, TRPV3, TRPV4, hERG, and NaV1.2 channels (IC50 >10 μM). Does not display any significant binding to 41 other receptors, ion channels, and transporters nor functional modulation of 7 enzymes that are known to modulate pain signaling.

Canonical smiles

CC(C)C1=CC=C(C=C1)NC(=O)CN2C=NC3=C2C(=O)N(C(=O)N3C)C

InChi

InChI=1S/C18H21N5O3/c1-11(2)12-5-7-13(8-6-12)20-14(24)9-23-10-19-16-15(23)17(25)22(4)18(26)21(16)3/h5-8,10-11H,9H2,1-4H3,(H,20,24)

InChiKey

HEQDZPHDVAOBLN-UHFFFAOYSA-N

IUPAC Name

2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(4-propan-2-ylphenyl)acetamide

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
Ambient
Storage information
The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

TRPA1 also known as the transient receptor potential ankyrin 1 is a non-selective cation channel with a mass of approximately 128 kDa. This protein is widely expressed in sensory neurons especially in dorsal root ganglia and trigeminal ganglia. TRPA1 is known for its activation by various physical and chemical stimuli including temperature mechanical forces and naturally occurring compounds like allicin found in garlic and allyl isothiocyanate from mustard oil. Compounds like diallyl trisulfide diallyl disulfide and polygodial have also been reported to activate TRPA1 and it plays a role in the perception of pain.
Biological function summary

TRPA1 contributes significantly to the sensation of pain and irritation. Functioning as a part of a receptor complex on the cellular membrane it integrates environmental stimuli to trigger responses such as pain and inflammation. TRPA1 interacts with various ligands which can modulate its activity leading to the perception of noxious cold and harsh chemical conditions. Recent studies also revealed its involvement in bronchial conditions implicating compounds like eucalyptol and related derivatives in modulating its effects.

Pathways

TRPA1 interacts with several critical sensory pathways involved in pain and thermosensation. It is an important player within the neurogenic inflammation pathway and the nociceptive pathway. In these pathways TRPA1 often acts together with related proteins like TRPV1 further modulating the response to heat and capsaicin. These interactions suggest a complex interplay between different TRP channels influencing how organisms react to different harmful stimuli.

TRPA1 is associated with inflammatory pain conditions and respiratory diseases like asthma. The regulation of TRPA1 activity can influence the progression of these conditions offering potential therapeutic targets. Its connection to TRPV1 in these diseases highlights the synergy between these receptors in managing pain and inflammation. Therefore targeting TRPA1 and its related proteins could help develop treatments aimed at alleviating symptoms linked to these disorders.

Product protocols

Publications (8)

Recent publications for all applications. Explore the full list and refine your search

Acta neuropathologica communications 13:70 PubMed40186313

2025

TRPA1 exacerbates selective retinal ganglion cell vulnerability under acute ocular hypertension.

Applications

Unspecified application

Species

Unspecified reactive species

Wenhan Lu,Yu Wang,Wei Hu,Xinyi Lin,Xiaoyu Tong,Yi Tian,Yuning Chen,Yicong Wang,Yan Xiao,Hongfang Yang,Yi Feng,Xinghuai Sun

ACS pharmacology & translational science 7:236-248 PubMed38230281

2024

Optogenetic Activation of Peripheral Somatosensory Neurons in Transgenic Mice as a Neuropathic Pain Model for Assessing the Therapeutic Efficacy of Analgesics.

Applications

Unspecified application

Species

Unspecified reactive species

Hao-Hao Chen,Muhammad Mohsin,Jia-Yi Ge,Yu-Ting Feng,Jing-Ge Wang,Yu-Sen Ou,Zuo-Jie Jiang,Bo-Ya Hu,Xing-Jun Liu

Molecules (Basel, Switzerland) 27: PubMed36364346

2022

Phytocannabinoid Compositions from Cannabis Act Synergistically with PARP1 Inhibitor against Ovarian Cancer Cells In Vitro and Affect the Wnt Signaling Pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Nurit Shalev,Michelle Kendall,Seegehalli M Anil,Sudeep Tiwari,Hadar Peeri,Navin Kumar,Eduard Belausov,Ajjampura C Vinayaka,Hinanit Koltai

Cancers 13: PubMed33916466

2021

Specific Compositions of Compounds Have Cytotoxic Activity and Inhibit Motility and Colony Formation of Human Glioblastoma Cells In Vitro.

Applications

Unspecified application

Species

Unspecified reactive species

Hadar Peeri,Nurit Shalev,Ajjampura C Vinayaka,Rephael Nizar,Gila Kazimirsky,Dvora Namdar,Seegehalli M Anil,Eduard Belausov,Chaya Brodie,Hinanit Koltai

Molecules (Basel, Switzerland) 26: PubMed33477303

2021

Cannabis-Derived Compounds Cannabichromene and Δ9-Tetrahydrocannabinol Interact and Exhibit Cytotoxic Activity against Urothelial Cell Carcinoma Correlated with Inhibition of Cell Migration and Cytoskeleton Organization.

Applications

Unspecified application

Species

Unspecified reactive species

Omer Anis,Ajjampura C Vinayaka,Nurit Shalev,Dvora Namdar,Stalin Nadarajan,Seegehalli M Anil,Ofer Cohen,Eduard Belausov,Jacob Ramon,Einav Mayzlish Gati,Hinanit Koltai

Scientific reports 11:1462 PubMed33446817

2021

Cannabis compounds exhibit anti-inflammatory activity in vitro in COVID-19-related inflammation in lung epithelial cells and pro-inflammatory activity in macrophages.

Applications

Unspecified application

Species

Unspecified reactive species

Seegehalli M Anil,Nurit Shalev,Ajjampura C Vinayaka,Stalin Nadarajan,Dvora Namdar,Eduard Belausov,Irit Shoval,Karthik Ananth Mani,Guy Mechrez,Hinanit Koltai

Frontiers in physiology 8:272 PubMed28515697

2017

TRPA1 Channels Modify TRPV1-Mediated Current Responses in Dorsal Root Ganglion Neurons.

Applications

Unspecified application

Species

Unspecified reactive species

Takayoshi Masuoka,Makiko Kudo,Yuka Yamashita,Junko Yoshida,Noriko Imaizumi,Ikunobu Muramatsu,Matomo Nishio,Takaharu Ishibashi

British journal of pharmacology 168:785-93 PubMed22928888

2012

Hydrogen sulphide-mediated vasodilatation involves the release of neurotransmitters from sensory nerves in pressurized mesenteric small arteries isolated from rats.

Applications

Unspecified application

Species

Unspecified reactive species

Benjamin J O White,Paul A Smith,William R Dunn
View all publications

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