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 Peso molecular: 355.39 Número EC: 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

Descripción general

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

Sinónimos

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

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

GATING INHIBITOR

Mecanismo de acción

Gating inhibitor of TRPA1

Nombres e identificadores

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

Objetivos asociados (humanos)

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)

Propiedades químicas y físicas

• Índice de refracción: 1.65
• Punto de ebullición (°C): 650.65° C
• Punto de fusión (°C): 221-223°C

Referencias

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]