| Bioactivity | NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC50 of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease[1]. |
| Target | NLRP3 inflammasome |
| Invitro | NLRP3-IN-12 (化合物 6E) (0.5-2 μM; 预处理 1 h) 抑制 THP-M 细胞中 LPS/ATP 刺激的裂解 caspase-1 和 IL-1β 的表达[1]。NLRP3-IN-12 (2 μM) 抑制 THP-M 细胞中的 GSDMD 介导的凋亡[1]。NLRP3-IN-12 (1 μM) 在人和大鼠肝微粒体中的半衰期 (T1/2) 分别为 53.4 min 和 31.8 min[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | NLRP3-IN-12 (化合物 6E) (5-10 mg/kg; i.p. daily for 10 d) 减弱小鼠 DSS 诱导的结肠炎[1]。NLRP3-IN-12 (20 mg/kg; i.v.) 在大鼠体内半衰期 (T1/2) 为 6.64 h，消除速率常数 (Kel) 为 0.107 h，清除率 (CL) 为 105 mL/kg/min，稳态的表观分布体积 (Vdss) 为 23.1 L/kg[1]。 Animal Model: |
| Name | NLRP3-IN-12 |
| Formula | C27H32ClNO7 |
| Molar Mass | 518.00 |
| 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]. Pang L, et, al. Development of novel oridonin analogs as specifically targeted NLRP3 inflammasome inhibitors for the treatment of dextran sulfate sodium-induced colitis. Eur J Med Chem. 2023 Jan 5;245(Pt 2):114919. |