HC-030031 - Moligand™, 10mM in DMSO , Gating inhibitor of TRPA1, CAS No.349085-38-7, Gating inhibitor of TRPA1

CAS: 349085-38-7 Cat. No.: H408813 Molecular Weight: 355.39 EC Number: 631-548-4

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

TOSLAB 829227 | 7H-Purine-7-acetamide, 1,2,3,6-tetrahydro-1,3-dimethyl-N-[4-(1-methylethyl)phenyl]-2,6-dioxo-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

HC-030031 HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively.
In vitro

HC-030031 is a substituted theophylline derivative. Potent and selective TRPA1 inhibitor. HC-030031 can block both inward and outward currents elicited by AITC or formalin rapidly and reversibly and also blocks the activation of TRPA1 by N-methylmaleimide and by electrophillic prostaglandins. It does not block currents mediated by TRPV1, TRPV3, TRPV4 hERG, or NaV1.2 channels.

In vivo

HC-030031 can be delivered to animals orally, by inhalation, or by injection. Oral administration (100 mg/kg) of HC-030031 significantly reversed mechanical hypersensitivity in rat models of chronic inflammatory or neuropathic pain, while local injection (100 μg) into inflamed mouse hind paws attenuated mechanical, but not heat, hypersensitivity. ^{[2] [3]}
Cell Data

cell lines：KB3-1, KBV-1, Hela, and Hs578T cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

TOSLAB 829227 | 7H-Purine-7-acetamide, 1, 2, 3, 6-tetrahydro-1, 3-dimethyl-N-[4-(1-methylethyl)phenyl]-2, 6-dioxo-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

GATING INHIBITOR

Mechanism of action

Gating inhibitor of TRPA1

Names and Identifiers

• Isomeric SMILES: CC(C)C1=CC=C(C=C1)NC(=O)CN2C=NC3=C2C(=O)N(C(=O)N3C)C
• WGK Germany: 3
• Molecular Weight: 355.39
• Reaxy-Rn: 12759009
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12759009&ln=

Associated Targets(Human)

TRPA1 Tclin Transient receptor potential cation channel subfamily A member 1 (11 Activities)

Discover Target: TRPA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Refractive Index: 1.65
• Boil Point(°C): 650.65° C
• Melt Point(°C): 221-223°C

References

1. Jingyun Ding, Huiyan Wang, Zequn Li, Jiangnan Sun, Peng Ding, Xiaomei Chi, Mingfang Yang, Yaqing Chang, Chong Zhao.  (2022)  Digestive Enzyme Activities and Gut Emptying Are Correlated with the Reciprocal Regulation of TRPA1 Ion Channel and Serotonin in the Gut of the Sea Urchin Strongylocentrotus intermedius.  Biology-Basel,  11  (4): (503).  [PMID:35453703] [10.3390/biology11040503]