NP3-146 sodium is a NLRP3 inflammasome inhibitor through locking the NACHT domain of NLRP3. NP3-146 sodium shows potent inhibitory activity against IL-1β release with an IC50 value of 0.171 μM in LPS /Nigericin -stimulated BMDM cells. NP3-146 sodium regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants. NP3-146 sodium can be used for the research of inflammatory diseases [1] [2].
In Vitro, NP3-146 (1-10000 nM) sodium significantly inhibits IL-1β release with an IC50 value of 171 nM[1]. NP3-146 (0.05-0.5 μM) sodium regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants of the BMDM cells[1].
References:
[1]. Feng H, et al. Design, synthesis and biological evaluation of sulfonylurea derivatives as NLRP3 inflammasome inhibitors. Bioorg Med Chem Lett. 2024 Dec 1;114:129987.
[2]. Harrison D, et al. Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors. ACS Med Chem Lett. 2022 Aug 1;13(8):1321-1328.
In Vitro, NP3-146 (1-10000 nM) sodium significantly inhibits IL-1β release with an IC50 value of 171 nM[1]. NP3-146 (0.05-0.5 μM) sodium regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants of the BMDM cells[1].
References:
[1]. Feng H, et al. Design, synthesis and biological evaluation of sulfonylurea derivatives as NLRP3 inflammasome inhibitors. Bioorg Med Chem Lett. 2024 Dec 1;114:129987.
[2]. Harrison D, et al. Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors. ACS Med Chem Lett. 2022 Aug 1;13(8):1321-1328.