2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Pyroptosis Interleukin Related
  4. NLRP3-IN-83

NLRP3-IN-83 是一种选择性且口服有效的 NLRP3 炎症小体激活抑制剂。NLRP3-IN-83 通过阻断 NLRP3 表现出良好的抑制 IL-1β 活性，其 IC50 为 1.4 μM，且不依赖 NF-κB 信号传导。NLRP3-IN-83 对 AIM2 炎症小体通路的抑制作用轻微，但对 NLRC4 炎症小体无影响。NLRP3-IN-83 预防了细胞焦亡 (pyroptosis)，并且在溃疡性结肠炎模型中表现出显著的抗炎功效。NLRP3-IN-83 可用于炎症性肠病 (IBD) 的研究。

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NLRP3-IN-83

NLRP3-IN-83 Chemical Structure

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Customer Review

NLRP3-IN-83 相关抗体

Top Publications Citing Use of Products

查看 NOD-like Receptor (NLR) 亚型特异性产品:

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NLRP3 NLRP1 NOD1 NOD2

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-83 is a selective and orally active NLRP3 inflammasome activation inhibitor. NLRP3-IN-83 exhibits good inhibitory IL-1β activity with an IC50 of 1.4 μM by blocking NLRP3, independent of NF-κB signaling. NLRP3-IN-83 only slightly inhibits AIM2 inflammasome pathway, but has no effect on NLRC4 inflammasome. NLRP3-IN-83 prevent cell pyroptosis and exhibits significant anti-inflammatory efficacy in ulcerative colitis model. NLRP3-IN-83 can be used for the study of inflammatory bowel disease (IBD)[1].

IC50 & Target[1]

NLRP3 inflammasome

 

IL-1β

1.4 μM (IC50)

体外研究
(In Vitro)

NLRP3-IN-83 (Compound 10) (0.625-5 μM, 1-25 h) 在 LPS (HY-D1056) 预处理的 J774A.1 细胞、LPS 预处理的小鼠 BMDMs 细胞 (使用 Nigericin (HY-127019) 或 SiO2 刺激) 以及 PMA (HY-18739) 诱导分化的人 THP-1 巨噬细胞模型中，均能显著抑制 IL-1β 的释放，且呈现浓度依赖性[1]。
NLRP3-IN-83 (1-5 μM, 2 h) 显著降低 LPS 预处理的 J774A.1 细胞上清中 caspase-1 (p20) 和 IL-1β 的水平，同时不影响细胞内 pro-caspase-1、pro-IL-1β、NLRP3 和 ASC 的表达水平[1]。 NLRP3-IN-83 (1-5 μM) 通过抑制 GSDMD 的切割和减少 LDH 的释放，能够有效预防 LPS 预处理的 J774A.1 细胞发生焦亡[1]。
NLRP3-IN-83 (2.5-10 μM, 24 h) 对 J774A.1 巨噬细胞和人胚胎肾细胞 HEK-293T 均未显示出显著毒性[1]。
NLRP3-IN-83 (1-5 μM, 2-6 h) 能够抑制 NLRP3 炎症小体的激活，同时对 NF-κB 信号通路没有显著影响[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NLRP3-IN-83 相关抗体:

ELISA Assay[1]

Cell Line: LPS-primed J774A.1 or BMDMs, THP-1 cells
Concentration: 0.625, 1.25 and 2.5 μM (J774A.1 cells); 1,2, and 5 μM (others)
Incubation Time: 1 h and stimulated with Nigericin for 1 h; with SiO2 for 8 h; with PMA for 24 h
Result: Significantly inhibited the release of IL-1β, showing a clear concentration-dependent effect.

Western Blot Analysis[1]

Cell Line: LPS-primed J774A.1 cells
Concentration: LPS-primed J774A.1 cells
Incubation Time: 1 h and stimulated with Nigericin for 1 h
Result: Reduced the production of caspase-1 (p20) and decreased the level of mature IL-1β (p17).
Did not affect the expression levels of pro-caspase-1, pro-IL-1β, NLRP3 and ASC.
Inhibited the self-oligomerization process of NLRP3.
Reduced the binding of NLRP3 to the adaptor protein ASC.
Significantly inhibited the formation of ASC oligomers.
体内研究
(In Vivo)

NLRP3-IN-83 (Compound 10) (10-20 mg/kg, i.g., 每日一次，连续 7 天) 在 DSS (HY-116282C) 诱导的溃疡性结肠炎模型中表现出显著的抗炎效果[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DSS-induced ulcerative colitis model established in 6-8-week-old C57BL/6 mice[1]
Dosage: 10 and 20 mg/kg
Administration: Intragastric administration (i.g.), once daily for 7 days
Result: Significantly improved symptoms of weight loss and rectal bleeding and shortening.
Significantly alleviated the pathological changes in the tissue (such as mucosal ulcers, crypt loss, inflammatory infiltration, etc.).
Dose-dependently reduced IL-1β, down-regulated NLRP3 and caspase-1 expression.
分子量

280.32

Formula

C17H16N2O2
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.
纯度 & 产品资料
参考文献

NLRP3-IN-83 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NLRP3-IN-83NOD-like Receptor (NLR)PyroptosisInterleukin RelatedILHydroxyquinolineInflammasomeIL-1βInflammatory bowel diseaseInhibitorinhibitorinhibit

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