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MCC950 (sodium)研究進展

發(fā)布日期:2017-11-01   瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/MCC950-sodium.htmlMCC950 (sodium)/a產(chǎn)品描述:MCC950 sodium is a potent, selective
MCC950 (sodium)產(chǎn)品描述:MCC950 sodium is a potent, selective NLRP3 inhibitor with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.IC50 & Target: IC50: 7.5 nM (NLRP3, in BMDMs), 8.1 nM (NLRP3, in HMDMs)[1]In Vitro: MCC950 blocks canonical and non-canonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibits NLRP3 but not AIM2, NLRC4 or NLRP1 activation. The effect of MCC950 on NLRP3 inflammasome activation is tested in mouse bone marrow derived macrophages (BMDM) and human monocyte derived macrophages (HMDM). The IC50 of MCC950 in BMDM is approximately 7.5 nM, while in HMDM it has a similar inhibitory capacity (IC50=8.1 nM). MCC950 also dose dependently inhibit IL-1β but not TNF-α secretion.MCC950 specifically blocks caspase-11-directed NLRP3 activation and IL-1β secretion upon stimulation of the non-canonical pathway. NLRC4-stimulated IL-1β and TNF-α secretion (as activated by Salmonella typhimuri


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