| Bioactivity | NLRP3-IN-39 (Compound 49) inhibits the assembly and activation of NLRP3 inflammatory vesicles. NLRP3-IN-39 exerts its inhibitory effect by covalently binding to Cys 279 of the NLRP3 protein. NLRP3-IN-39 inhibits Nigericin (HY-127019)-induced IL-1β release from THP-1 cells (IC50= 0.29 μM)[1]. |
| Invitro | NLRP3-IN-39 在多种细胞类型中均可以抑制 Nigericin (HY-127019) 诱导的 IL-1β 释放，IC50 分别是 0.29 μM (THP-1), 44.97 nM (PBMCs), 738.8 nM (BMDMs)[1]。NLRP3-IN-39 (0-1 μM; 24 h) 在 THP- 1细胞和 BMDMs 中有效抑制了炎症因子的分泌，而不影响前体蛋白的表达[1]。NLRP3-IN-39 (0-1 μM; 40 min) 在 THP-1 细胞和 BMDMs 中显著抑制了 NLRP3 炎症小体激活引起的 LDH 释放，抑制了细胞焦亡。在 LPS 预处理的 THP-1 细胞中，显著浓度依赖性的抑制 Nigericin 刺激引起的 IL-1β 释放[1]。NLRP3-IN-39 (1 μM; 24 h) 在 Nigericin 诱导的 THP-1 细胞中减少 ASC 寡聚体和 ASC specks 形成，NLRP3 KO THP-1 细胞则没有这种现象[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NLRP3-IN-39 相关抗体: Western Blot Analysis[1] Cell Line: |
| In Vivo | NLRP3-IN-39 (15, 30 mg/kg; i.p.; 单剂量) 在 DSS 诱导的溃疡性结肠炎小鼠模型中展示了显著的抗炎作用[1]。NLRP3-IN-39 在 5% DMSO 和 95% 盐水中制备至 3 mg/mL 的浓度。在 C57BL/6 小鼠中的药代动力学分析[1] Route |
| Formula | C21H21Cl2NO4 |
| Molar Mass | 422.30 |
| 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]. Zhao M, et al. Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. J Med Chem. 2024 May 9;67(9):7516-7538. |