NLRP3-IN-12 是一种特异性的NLRP3炎症小体抑制剂。NLRP3-IN-12 通过靶向 NLRP3 蛋白抑制 IL-1β 的释放，IC50值为 0.45 μM。NLRP3-IN-12 可用于研究炎症性肠病。
| 生物活性 | NLRP3-IN-12 is a specificNLRP3inflammasomeinhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting theNLRP3protein, with anIC50of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease[1]. |
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体外研究
(In Vitro) | 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: | THP-M cells | | Concentration: | 0.5, 1, 2 μM | | Incubation Time: | Pretreated for 1 h, then stimulated with LPS (1 μg/mL) for 4.5 h, and ATP (5 mM) for 0.5 h. | | Result: | Reduced the secretion of IL-1β and caspase-1.
Had no effect on the levels of NLRP3, pro-IL-1β, ASC, pro-caspase 1, p65, p-p65, IκBα, and p-IκBα. |
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体内研究
(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: | C57BL/6 mice were induced acute colitis by drinking 3% DSS (dextran sulfate sodium)[1] | | Dosage: | 5, 10 mg/kg | | Administration: | Intraperitoneal injection daily for 10 days in aqueous solution containing DMSO/0.5% CMC-Na/normal saline | | Result: | Attenuated DSS-induced weight loss, loose stools, bloody stools, shortened colons, increased disease activity index score, and lower survival rate. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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