| Bioactivity | NLRP3-IN-16 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-16 inhibits IL-1β release with an IC50 of 0.065 μM. NLRP3-IN-16 can be used for the research of inflammation[1]. |
| Invitro | NLRP3-IN-16 (化合物 12d) 抑制 IL-1β 释放，IC50 为 0.065 μM (ELISA 测定) [1]。NLRP3-IN-16 (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-16 通过抑制 ASC 寡聚化来抑制 NLRP3 炎性体复合物的形成[1]。NLRP3-IN-16 在人和小鼠肝微粒体中表现出代谢稳定性 (T1/2: 223.5 min; Clint: 6.2act μL/min/mg)[1]. Western Blot Analysis[1] Cell Line: |
| In Vivo | NLRP3-IN-16 (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-16 |
| Formula | C25H25NO5 |
| Molar Mass | 419.47 |
| 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. |