Bioactivity | NLRP3-IN-17 is a potent, selective and orally active NLRP3 inflammasome inhibitor with an IC50 value of 7 nM. NLRP3-IN-17 significantly inhibits NLRP3 dependent IL-1β secretion in mice and can be used for chronic inflammatory diseases research[1]. |
In Vivo | NLRP3-IN-17 (3 mg/kg; po) 显示良好的PK 数据,AUC、t1/2 和 F% 值分别为 4.2 μg.h/mL、2.91 h 和 56%[1]。 NLRP3-IN-17 (10 mg/kg; P.O.; 单剂量) 显著抑制 NLRP3 依赖性 IL-1β 的分泌,使急性体内 LPS+ATP 刺激模型雌性 C57BL/6 小鼠 IL-1β 水平降低了44%[1]。 |
Name | NLRP3-IN-17 |
CAS | 2254432-75-0 |
Formula | C21H22N4O2S |
Molar Mass | 394.49 |
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]. Sameer Agarwal, et al. Discovery of N-Cyano-sulfoximineurea Derivatives as Potent and Orally Bioavailable NLRP3 Inflammasome Inhibitors. ACS Med Chem Lett. 2020 Feb 27;11(4):414-418. |