2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Interleukin Related Caspase
  4. NLRP3-IN-91

NLRP3-IN-91 是一种强效的 NLRP3 炎症小体抑制剂，其 Kd 值为 558.4 nM。NLRP3-IN-91 直接靶向 NLRP3 的 NACHT 结构域，阻断炎症小体的组装与激活，并发挥抗炎作用。NLRP3-IN-91 可延长 LPS (HY-D1056) 诱导的脓毒症小鼠模型的存活时间。NLRP3-IN-91 可用于脓毒症的研究。

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NLRP3-IN-91

NLRP3-IN-91 Chemical Structure

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NLRP3-IN-91 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 IL-18

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-91 is a potent NLRP3 inflammasome inhibitor with a Kd of 558.4 nM. NLRP3-IN-91 directly targets the NLRP3 NACHT domain, blocks inflammasome assembly and activation, and exerts anti-inflammatory effects. NLRP3-IN-91 increases survival time in a murine model of LPS (HY-D1056)-induced sepsis. NLRP3-IN-91 can be used for the research of sepsis[1].

IC50 & Target[1]

NLRP3 inflammasome

558.4 nM (Kd)

IL-1β

0.094 μM (IC50)

Caspase-1

 

体外研究
(In Vitro)

NLRP3-IN-91 (compound D12) (0.04-10 μM; 30 min) 可强效抑制 J774A.1 小鼠巨噬细胞中 NLRP3 炎症小体介导的 IL-1β 分泌，其 IC50 为 0.094 μM[1]。
NLRP3-IN-91 (24 h) 体外显示出低细胞毒性，在 J774A.1 小鼠巨噬细胞中的 CC50 值 > 30 μM，在 AML-12 小鼠正常肝细胞中的 CC50 值 > 100 μM[1]。
NLRP3-IN-91 (0.2-5 μM; 2.5 h) 可通过减少剪切型半胱天冬酶-1 (p20) 和成熟 IL-1β 的产生，以剂量依赖方式抑制 J774A.1 小鼠巨噬细胞中 NLRP3 炎症小体的组装与激活[1]。

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

NLRP3-IN-91 相关抗体:

ELISA Assay[1]

Cell Line: J774A.1 murine macrophages
Concentration: 0.04, 0.12, 0.37, 1.11, 3.33, 10 μM
Incubation Time: 30 min
Result: Inhibited IL-1β secretion by 80.2% at 1 μM.
Inhibited IL-1β secretion by 96.6% at 10 μM.
Exhibited an IC50 of 0.094 μM for NLRP3 inflammasome-mediated IL-1β release.

Western Blot Analysis[1]

Cell Line: J774A.1 murine macrophages
Concentration: 0.2, 1, and
5 μM
Incubation Time: 2.5 h
Result: Suppressed the production of cleaved caspase-1 (p20 subunit) and mature IL-1β in a dose-dependent manner.
Did not affect levels of pro-caspase-1, pro-IL-1β, NLRP3, or GAPDH.
体内研究
(In Vivo)

NLRP3-IN-91 (compound D12) (10 mg/kg；腹腔注射；单次给药；LPS 预处理 1 小时) 可显著延长 LPS 诱导的脓毒症小鼠的存活时间[1]。

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

Animal Model: Male C57BL/6 mice (8 weeks old, 20-25 g) intraperitoneally injected with LPS (40 mg/kg)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose; 1 hour pre-LPS
Result: Exceeded 40% survival rate at 72 hours post-LPS challenge.
分子量

576.04

Formula

C27H27ClFN3O6S
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-91 相关分类

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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-91NOD-like Receptor (NLR)Interleukin RelatedCaspaseILNLRP3 inflammasomemurine modelNLRP3 NACHT domainAML-12 mouse normal hepatocytesAIM2 inflammasomeIL-1βC57BL/6 miceTNF-αJ774A.1 murine macrophagesLPS-induced sepsisInhibitorinhibitorinhibit

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