Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 229 | 现货 | ||
10 mg | ¥ 373 | 现货 | ||
50 mg | ¥ 996 | 现货 | ||
100 mg | ¥ 1,497 | 待询 | ||
200 mg | ¥ 1,997 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 411 | 现货 |
产品描述 | HC-030031 (TOSLAB 829227) is a potent TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively. |
靶点活性 | AITC--evoked calcium influx:6.2±0.2 μM, formalin-evoked calciμM influx:5.3±0.2 μM |
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。 |
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. |
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]. |
动物实验 | Animal Models: Male Sprague-Dawley rats. Formulation: 0.5% Methylcellulose. Dosages: 100,300 mg/kg. Administration: oral administration |
别名 | 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺, HC030031, TOSLAB 829227 |
分子量 | 355.39 |
分子式 | C18H21N5O3 |
CAS No. | 349085-38-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8138 mL | 14.0691 mL | 28.1381 mL | 70.3453 mL |
5 mM | 0.5628 mL | 2.8138 mL | 5.6276 mL | 14.0691 mL | |
10 mM | 0.2814 mL | 1.4069 mL | 2.8138 mL | 7.0345 mL | |
20 mM | 0.1407 mL | 0.7035 mL | 1.4069 mL | 3.5173 mL | |
50 mM | 0.0563 mL | 0.2814 mL | 0.5628 mL | 1.4069 mL | |
100 mM | 0.0281 mL | 0.1407 mL | 0.2814 mL | 0.7035 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
HC-030031 349085-38-7 Membrane transporter/Ion channel TRP/TRPV Channel TRP Channel 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺 HC030031 Transient receptor potential channels TOSLAB 829227 Inhibitor HC 030031 TOSLAB829227 inhibit TOSLAB-829227 inhibitor