| Identification | Back Directory | [Name]
1H-Benzimidazole, 1-ethyl-5-methyl-2-phenyl- | [CAS]
960119-75-9 | [Synonyms]
1H-Benzimidazole, 1-ethyl-5-methyl-2-phenyl- | [Molecular Formula]
C16H16N2 | [MOL File]
960119-75-9.mol | [Molecular Weight]
236.31 |
| Hazard Information | Back Directory | [Description]
Fc11a-2 is a specific inhibitor of inflammasome assembly, targeting the NLRP3 inflammasome by interfering with the proximity-induced autocleavage of procaspase-1. | [Uses]
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]. | [in vivo]
Fc 11a-2 (3-30 mg/kg; Orally; from day 1 to day 10) dose-dependently attenuates the loss of body weight and shortening of colon length induced by DSS[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.
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| [References]
[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. DOI:10.3390/molecules22020213
[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. DOI:10.1016/j.bcp.2013.03.008
[3] Biswadeep Das, et al. Promise of the NLRP3 Inflammasome Inhibitors in In Vivo Disease Models. Molecules. 2021 Aug 18;26(16):4996. DOI:10.3390/molecules26164996 |
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