PeptideDB

NLRP3-IN-14

CAS: 2767369-80-0 F: C27H28N2O4 W: 444.52

NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release w
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Bioactivity NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation[1].
Invitro NLRP3-IN-14 (化合物 5j) 抑制 IL-1β 释放,IC50 为 0.131 μM (ELISA 测定) [1]。NLRP3-IN-14 (2 μM,3 小时) 抑制小鼠腹膜巨噬细胞 (PM) 中 IL-1β (p17) 和 caspase-1 (p20) 的分泌[1]。NLRP3-IN-14 通过抑制 ASC 寡聚化来抑制 NLRP3 炎性体复合物的形成[1]。NLRP3-IN-14 (10 μM,5 小时) 随着温度升高抑制蛋白质 NLRP3 的降解[1]。NLRP3-IN-14 在人和小鼠肝微粒体中表现出代谢稳定性 (T1/2: 866.3 min; Clint: 1.6 μL/min/mg)[1]. Western Blot Analysis[1] Cell Line:
In Vivo NLRP3-IN-14 (化合物 5j) (50 mg/kg;i.p.) 在败血症小鼠模型中表现出抗炎作用[1]。 Animal Model:
Name NLRP3-IN-14
CAS 2767369-80-0
Formula C27H28N2O4
Molar Mass 444.52
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]. Li J, et al. Scaffold Hybrid of the Natural Product Tanshinone I with Piperidine for the Discovery of a Potent NLRP3 Inflammasome Inhibitor. J Med Chem. 2023 Feb 23;66(4):2946-2963.