|2-(2-氯苄基)丙烯酸乙酯|CsnPharm

CAS No.: 866028-26-4

INF39/2-(2-氯苄基)丙烯酸乙酯 Catalog No. CSN22257

Synonyms: INF39

INF39 is an irreversible NLRP3 inhibitor with IC50 value of ~100 μM for inhibiton of NLRP3 ATPase, which can inhibit IL-1β release, caspase activation and pyroptosis in THP-1 cells.

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技术信息

生物活性

描述Nucleotide-binding oligomerization domain leucine rich repeat and pyrin domain-containing protein 3 (NLRP3) inflammasome is pivotal in maintaining intestinal homeostasis and sustaining enteric immune responses in the setting of inflammatory bowel diseases^[1]. INF39 is an irreversible and noncytotoxic NLRP3 inhibitor. INF39 is able to significantly inhibit ATP- and nigericin-induced IL-1β release at 10 μM. INF39 reduces caspase-1 activation and pyroptosis in the macrophages. INF39 can block not only NLRP3 activation but also the NF-κB pathway. INF39 potentially reacts with Cys-SH residues in the active site of cysteine protease caspase-1, but does not directly target caspase-1 activity. INF39 is able to reduce the steady state (or basal) BRET signal of NLRP3 without affecting the viability of cells, meaning that it can interfere with the basal NLRP3 conformation. INF39 does not block the initial conformational changes suffered by NLRP3 upon sensing the decrease of intracellular K+; however, it affects a second step of NLRP3 conformational change that could be related with the ATPase activity of the receptor and be independent of the decrease of intracellular K+. Oral administration of INF39 reduces systemic and colonic inflammation in rats treated with 2,4- dinitrobenzenesulfonic acid. Significant increments of body weight are observed in inflamed rats under treatment with INF39 (12.5, 25, and 50 mg/ kg). Treatment with DNBS results in a significant increment of spleen weight (+39.3%). Such an increase is significantly 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 dose-dependently attenuates the decrease in colonic length (−19, −13 and −8% at 12.5, 25, 50 mg/kg, respectively). Rats treated with INF39 displays 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). Oral administration of INF39 reduces colonic myeloperoxidase, IL-1β, and TNF Levels in DNBS-treated rats^[2].
参考文献

[1] Carolina Pellegrini,et al. A Comparative Study on the Efficacy of NLRP3 Inflammasome Signaling Inhibitors in a Pre-clinical Model of Bowel Inflammation. Front Pharmacol. 2018 Dec 3;9:1405.
[2] Cocco M, et al. Development of an Acrylate Derivative Targeting the NLRP3 Inflammasome for the Treatment of Inflammatory Bowel Disease.J Med Chem. 2017 May 11;60(9):3656-3671.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.4507 mL
- 22.2535 mL
- 44.5071 mL
- 5 mM
- 0.8901 mL
- 4.4507 mL
- 8.9014 mL
- 10 mM
- 0.4451 mL
- 2.2254 mL
- 4.4507 mL

技术信息

CAS号

866028-26-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H13ClO2

运输

蓝冰

分子量

224.68

别名

INF39

溶解度

DMSO	1.0 mg/mL (4.5 mM) warming

动物实验配方

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INF39/2-(2-氯苄基)丙烯酸乙酯 Catalog No. CSN22257

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