2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. NLRP3-IN-8

NLRP3-IN-8 (compound 27) 是具有口服活性的、与 NLRP3 直接结合的 NLRP3 炎性体抑制剂，对 IL-1 β 的IC50 值为1.23 μM. NLRP3-IN-8 对肝微粒体具有良好的代谢稳定性 (t1/2 = 138.63 min)，几乎没有毒性 (against L02: IC50 > 100 μM) 。

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NLRP3-IN-8 Chemical Structure

NLRP3-IN-8 Chemical Structure

CAS No. : 2768650-56-0

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NLRP3-IN-8 相关抗体

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查看 NOD-like Receptor (NLR) 亚型特异性产品:

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NLRP3 NLRP1 NOD1 NOD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM)[1].

IC50 & Target

NLRP3

 

NLRP3 inflammasome

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
L02 IC50
> 100 μM
Compound: 27
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 35428012]
体外研究
(In Vitro)

NLRP3-IN-8 (compound 27) exhibits prominent anti-inflammatory activity with an IC50 of 1.23 μM[1].
NLRP3-IN-8 exhibits good metabolic stability through human liver microsomes (t1/2 = 138.63 min)[1].
NLRP3-IN-8 (0-10 μM, 1 h) significantly inhibits pyrolysis rate in a concentration-dependent manner[1].
NLRP3-IN-8 only inhibits the activation of NLRP3 inflammasomes, and could inhibit the activation of inflammasome by a variety of inducer[1].
NLRP3-IN-8 blocks NLRP3-induced ASC oligomerization[1].
NLRP3-IN-8 inhibits NLRP3 inflammasome assembly by blocking the interaction of NLRP3-NEK7 and NLRP3-ASC[1].

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

NLRP3-IN-8 相关抗体:

Western Blot Analysis[1]

Cell Line: BMDMs cells
Concentration: 0.5, 1, and 2 μM
Incubation Time: 30 min, pretreated with LPS (200 ng/mL) for 3 h
Result: Dose-dependently blocked IL-1 b secretion and caspase-1 cleavage at concentrations of 0.5-2 μM. Inhibited the maturation of intracellular caspase-1 (p20), and did not affect the expression of other constituent proteins of NLRP3 inflammasome, such as pro-IL-1 β, pro-caspase-1 (p45), NLRP3, ASC and NEK7.
体内研究
(In Vivo)

NLRP3-IN-8 (compound 27) (DSS-induced C57BL/6 male mice; 0-20 mg/kg; intragastric; once a day, 7 days) effectively alleviates the severity of DSS-induced colitis in mouse[1].

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

Animal Model: DSS-induced acute colitis model in C57BL/6 male mice[1].
Dosage: 20 mg/kg and 10 mg/kg dissolved in 0.5% sodium carboxymethyl cellulose aqueous solution.
Administration: Intragastric administration, once a day, 7 days.
Result: Reduced the weight loss during the onset of colitis in mice, and decreased the disease activity index (DAI) in a dose-dependent manner. Reduced colon shortening, pathological index score, the expression of TNF-a, IL-6 and IL-1 β in the tissues and inhibited the decrease of goblet cells.
分子量

420.41

Formula

C23H20N2O6
CAS 号
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-8 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-82768650-56-0NOD-like Receptor (NLR)BMDMsDSS-induced colitisNLRP3 inflammasomeInhibitorinhibitorinhibit

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