化合物HC030031 T6530

Product Introduction
Bioactivity


英文名: HC-030031

描述: HC-030031 (TOSLAB 829227) 是一种有效的TRPA1选择性抑制剂，拮抗福尔马林和AITC 诱发的钙流入，IC50分别为5.3±0.2和6.2±0.2μM。

细胞实验: HC-030031 is prepared in DMSO and stored, and then diluted with appropriate medium (DMSO 0.4%) before use[2]. HEK-293 cells stably expressing human TRPA1 are plated into 384-well plates at a density of 20,000 cells/well 24 hours prior to assaying. On the day of assay, cells are loaded with 4 μM Fluo-4 dye and 0.08% pluronic acid for 1 hour at room temperature in assay buffer consisting of Hank's balanced salt solution supplemented with 20 mM HEPES, 2.5 mM probenecid, and 4% TR-40. Calcium influx assays are performed using the Fluorometric Imaging Plate Reader (FLIPR) TETRA. Concentration-response curves are generated for the TRPA1 agonists cinnamaldehyde and AITC prior to antagonist testing so EC60 concentrations could be determined. Titrations of HC-030031 are made from a DMSO stock solution and DMSO is kept to a constant of 0.4% in the assay. The antagonist is incubated with the cells for 10 minutes before the addition of an EC60 concentration of either cinnamaldehyde (18 μM) or AITC (6 μM) and calcium influx is monitored for an additional 10 minutes[2].

激酶实验: The activity of specific TLR agonists is assessed using the secretory embryonic alkaline phosphatase (SEAP) reporter gene that is linked to NF-κB activation in response to TLR stimulation. Measurement of SEAP activity using the Quanti-blue substrate (InvivoGen) after TLR agonist treatment is carried out.

动物实验: Animal Models: Male Sprague-Dawley rats. Formulation: 0.5% Methylcellulose. Dosages: 100,300 mg/kg. Administration: oral administration

体外活性: 口服给药（100 mg/kg）的HC-030031显著逆转慢性炎症或神经性疼痛大鼠模型中的机械超敏反应,而局部注射（100 μg）至发炎的小鼠后爪,减弱机械性而非热性超敏反应.

体内活性: HC-030031可以快速阻断AITC或Formalin引起的内向和外向电流,也能抑制N-methylmaleimide和Electrophillic前列腺素引起的TRPA1激活。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 35.5 mg/mL (100 mM)


关键字: TRP Channel | Transient receptor potential channels | Inhibitor | HC-030031 | HC 030031 | TOSLAB829227 | inhibit | TOSLAB-829227

相关产品: Podocarpic acid | Pyr3 | Pyr10 | TRPC6-PAM-C20 | ML-SA1 | IA-Alkyne | Chembridge-5861528 | RQ-00203078 | ABT-239 | Evifacotrep

相关库: Ion Channel Inhibitor Library | ReFRAME Related Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途