Fc 11a-2

Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis[1][2][3].

Signaling Pathways >> Immunology/Inflammation >> NOD-like Receptor (NLR)

Research Areas >> Inflammation/Immunology

Fc 11a-2 (10 μM) 抑制用 ATP 激活的 LPS (HY-D1056) 引发的 THP-1 细胞中释放 IL-1β 和 IL-18，IC50 约 10 μM[1]。

Fc 11a-2 (3-30 mg/kg; 口服; 从第 1 天到第 10 天) 剂量依赖性地减轻由 DSS 诱导的体重减轻和结肠长度缩短[2]。 Animal Model: C57BL/6 mice induced Colitis with 2.5% DSS[2] Dosage: 3, 10, 30 mg/kg Administration: Orally; from day 1 to day 10 Result: Significantly attenuated the loss of body weight during the disease progression at 10 and 30 mg/kg. The myeloperoxidase (MPO) activity in colons at 10 and 30 mg/kg was lower than that of the vehicle-treated group. Significantly reduced the disease activity index, histopathologic scores and myeloperoxidase activity.

[1]. Liangkun Pan, et al. Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives and Analogs Targeting the NLRP3 Inflammasome. Molecules. 2017 Jan 30;22(2):213.  

[2]. Wen Liu, et al. A novel benzo[d]imidazole derivate prevents the development of dextran sulfate sodium-induced murine experimental colitis via inhibition of NLRP3 inflammasome. Biochem Pharmacol. 2013 May 15;85(10):1504-12.  

[3]. Biswadeep Das, et al. Promise of the NLRP3 Inflammasome Inhibitors in In Vivo Disease Models. Molecules. 2021 Aug 18;26(16):4996.