2. Immunology/Inflammation NF-κB
  3. NOD-like Receptor (NLR) Interleukin Related NF-κB NO Synthase
  4. NLRP3-IN-76

NLRP3-IN-76 是一种具有口服活性的 NLRP3 抑制剂。NLRP3-IN-76 可抑制 NO 的产生以及促炎细胞因子(iNOS、IL-6、IL-1β 和 TNFα) 的 mRNA 水平。NLRP3-IN-76 通过抑制 NLRP3 炎症小体和 NF-κB 信号通路的激活发挥抗炎作用。NLRP3-IN-76 可改善 DSS (HY-116282C) 诱发的结肠炎，并可用于炎症性肠病 (IBD) 的研究。

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NLRP3-IN-76 Chemical Structure

NLRP3-IN-76 Chemical Structure

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NLRP3-IN-76 相关抗体

Top Publications Citing Use of Products

查看 NOD-like Receptor (NLR) 亚型特异性产品:

查看所有亚型
NLRP3 NLRP1 NOD1 NOD2

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
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

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 NO Synthase 亚型特异性产品:

查看所有亚型
nNOS iNOS eNOS

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-76 is an orally active NLRP3 inhibitor. NLRP3-IN-76 inhibits the production of NO, and the mRNA levels of proinflammatory cytokines (iNOS, IL-6, IL-1β and TNFα). NLRP3-IN-76 shows anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome and NF-κB signaling pathway. NLRP3-IN-76 ameliorates DSS (HY-116282C)-induced colitis and can be used for research of inflammatory bowel diseases (IBD)[1].

体外研究
(In Vitro)

NLRP3-IN-76 (Compound ST12) (10 μM，24 小时) 可抑制 LPS 诱导的 RAW264.7 细胞中一氧化氮 (NO) 的产生 (52.67%)[1]。
NLRP3-IN-76 (10 μM，24 小时) 可抑制 LPS 刺激的 RAW264.7 细胞中促炎细胞因子的 mRNA 水平，例如诱导型一氧化氮合酶 (iNOS)、IL-6、IL-1β 和 TNF-α[1]。
NLRP3-IN-76 (2.5-10 μM, 24 h) 可抑制 LPS 刺激的 RAW264.7 细胞中 NLRP3 炎症小体活化和 NF-κB 信号通路的激活[1]。

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

NLRP3-IN-76 相关抗体:

RT-PCR[1]

Cell Line: LPS (0.1 μg/mL) induced RAW264.7 cells
Concentration: 2.5, 10 μM
Incubation Time: 24 h
Result: Significantly inhibited the mRNA levels of inflammatory factors (iNOS, IL-6, IL-1β and TNF-α) at 10 μM.
Inhibited the mRNA levels of IL-6, IL-1β at 2.5 μM.

Western Blot Analysis[1]

Cell Line: LPS (0.1 μg/mL) induced RAW264.7 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Dose-dependently downregulated the expression of p-IκBα and p-p65 without affecting IκBα and p65.
Downregulated the expression of NLRP3.
Inhibited the expression of caspase-1, IL-18 and GSDMD.
体内研究
(In Vivo)

NLRP3-IN-76 (Compound ST12) (35 mg/kg，灌胃，9 天) 通过抑制 NLRP3 炎症小体的体内激活来保护小鼠免受 DSS 诱发的结肠炎[1]。
NLRP3-IN-76 (100-400 mg/kg，口服) 在 C57 小鼠中耐受性良好 (LD50: 300 mg/kg)[1]。

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

Animal Model: 2.6 % DSS induced colitis in male C57BL/6 mice (6-7 weeks)[1]
Dosage: 35 mg/kg
Administration: Intragastric gavage (i.g.), 9 days
Result: Increased the colon lengths (6.09 cm) compared to the DSS-induced colitis model group (4.39 cm).
Alleviated the DSS-induced reduction in crypt numbers and depletion of goblet cells.
Reduced DSS-induced CD86-positive cells.
Reduced the p-IκBα and p-p65 levels in colonic tissues.
No significant organ toxicity was observed.
分子量

338.32

Formula

C17H14N4O4
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-76 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-76NOD-like Receptor (NLR)Interleukin RelatedNF-κBNO SynthaseILNuclear factor-κBNuclear factor-kappaBNitric oxide synthasesNOSProinflammatoryDSScolitisNLRP3 inflammasomeanti-inflammatoryinflammatory bowel diseasesIBDRAW264.7 cellInhibitorinhibitorinhibit

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