Powder: -20°C for 3 years | In solvent: -80°C for 1 year
INF39 是无细胞毒性的NLRP3不可逆抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 455 | 现货 | ||
2 mg | ¥ 863 | 现货 | ||
5 mg | ¥ 1,830 | 现货 | ||
10 mg | ¥ 2,730 | 现货 | ||
25 mg | ¥ 4,630 | 现货 | ||
50 mg | ¥ 6,590 | 现货 | ||
100 mg | ¥ 8,820 | 现货 | ||
500 mg | ¥ 17,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,970 | 现货 |
产品描述 | INF39 is a noncytotoxic and irreversible NLRP3 inhibitor. |
体外活性 | INF39 possibly reacts with Cys-SH residues in the active site of cysteine protease caspase-1 but does not directly inhibit caspase-1 activity. INF39 (10 μM) can markedly inhibit ATP- and nigericin-induced IL-1β release. In the macrophages, INF39 suppresses caspase-1 activation and pyroptosis. INF39 can also block the NF-κB pathway. INF39 can reduce the steady-state (or basal) BRET signal of NLRP3, and not affect the viability of cells. INF39 cannot affect the initial conformational changes suffered by NLRP3 upon sensing the decrease of intracellular K+, but it affects the second step of NLRP3 conformational change. INF39 reaches the intestinal epithelium without undergoing chemical modifications. It is likely to act locally at the mucosal epithelial level after absorption into epithelial cells. |
体内活性 | INF39 (p.o.) reduces systemic and colonic inflammation in rats treated with 2,4- dinitrobenzene sulfonic acid. In inflamed rats, INF39 (12.5/25/50 mg/ kg) markedly increases body weight. DNBS causes a significant increment of spleen weight (+39.3%). This increase is markedly reduced by administration of INF39 (+2.2, +4.3 and +4.8% at 12.5, 25, 50 mg/kg, respectively). The inhibition of NLRP3 inflammasome complex with INF39 can dose-dependently attenuate the decrease in colonic length (?19, ?13 and ?8% at 12.5, 25, 50 mg/kg, respectively). Rats treated with INF39 shows a significant reduction of macroscopic damage score (4.7 at 12.5 mg/kg, 3.1 at 25 mg/kg, and 2.8 at 50 mg/kg). |
细胞实验 | Human THP-1 cells were exposed to INF39 (0.1?100 μM, 72 h), and then cell viability was evaluated by the MTT assay. |
动物实验 | Animal Models: Male Sprague?Dawley rats. Solvent: olive oil. Dosages: 12.5,25.0,50.0 mg/kg/day,p.o. |
分子量 | 224.68 |
分子式 | C12H13ClO2 |
CAS No. | 866028-26-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (44.51 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.4508 mL | 22.2539 mL | 44.5077 mL | 111.2694 mL |
5 mM | 0.8902 mL | 4.4508 mL | 8.9015 mL | 22.2539 mL | |
10 mM | 0.4451 mL | 2.2254 mL | 4.4508 mL | 11.1269 mL | |
20 mM | 0.2225 mL | 1.1127 mL | 2.2254 mL | 5.5635 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。
INF39 866028-26-4 Immunology/Inflammation NF-Κb NOD-like Receptor (NLR) NOD inhibit INF 39 INF-39 Inhibitor inhibitor