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.
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- Molecules (Basel, Switzerland) 27:2022Phytocannabinoid Compositions from Cannabis Act Synergistically with PARP1 Inhibitor against Ovarian Cancer Cells In Vitro and Affect the Wnt Signaling Pathway.Applications:Unspecified applicationReactive species:Unspecified reactive speciesNurit Shalev,Michelle Kendall,Seegehalli M Anil,Sudeep Tiwari,Hadar Peeri,Navin Kumar,Eduard Belausov,Ajjampura C Vinayaka,Hinanit KoltaiPubMed 36364346
- Cancers 13:2021Specific Compositions of Compounds Have Cytotoxic Activity and Inhibit Motility and Colony Formation of Human Glioblastoma Cells In Vitro.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHadar Peeri,Nurit Shalev,Ajjampura C Vinayaka,Rephael Nizar,Gila Kazimirsky,Dvora Namdar,Seegehalli M Anil,Eduard Belausov,Chaya Brodie,Hinanit KoltaiPubMed 33916466
- Molecules (Basel, Switzerland) 26:2021Cannabis-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 applicationReactive species:Unspecified reactive speciesOmer Anis et. al.PubMed 33477303
- Scientific reports 11:14622021Cannabis compounds exhibit anti-inflammatory activity in vitro in COVID-19-related inflammation in lung epithelial cells and pro-inflammatory activity in macrophages.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSeegehalli M Anil et. al.PubMed 33446817
- Frontiers in physiology 8:2722017TRPA1 Channels Modify TRPV1-Mediated Current Responses in Dorsal Root Ganglion Neurons.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTakayoshi Masuoka,Makiko Kudo,Yuka Yamashita,Junko Yoshida,Noriko Imaizumi,Ikunobu Muramatsu,Matomo Nishio,Takaharu IshibashiPubMed 28515697
- British journal of pharmacology 168:785-932012Hydrogen sulphide-mediated vasodilatation involves the release of neurotransmitters from sensory nerves in pressurized mesenteric small arteries isolated from rats.Applications:Unspecified applicationReactive species:Unspecified reactive speciesBenjamin J O White,Paul A Smith,William R DunnPubMed 22928888
Key facts
- CAS number
- 349085-38-7
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 355.4 Da
- Molecular formula
- C18H21N5O3
- PubChem identifier
- 1150897
- Nature
- Synthetic
Target data
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
Recommended products
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.
Key facts
- CAS number
- 349085-38-7
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 355.4 Da
- Molecular formula
- C18H21N5O3
- PubChem identifier
- 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
Storage
- 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 info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
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.
- Associated diseases and disorders
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.
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Chemical Structure - HC-030031, TRPA1 blocker (ab120554)
2D chemical structure image of ab120554, HC-030031, TRPA1 blocker
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