| Bioactivity | 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]. |
| Invitro | 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]。 |
| In Vivo | 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: |
| Name | Fc 11a-2 |
| CAS | 960119-75-9 |
| Formula | C16H16N2 |
| Molar Mass | 236.31 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |