1. Immunology/Inflammation
  2. NOD-like Receptor (NLR)
  3. NLRP3-IN-16

NLRP3-IN-16 是一种有效的、选择性的 NLRP3 炎症小体抑制剂。NLRP3-IN-16 抑制 IL-1β 释放,IC50 为 0.131 μM。NLRP3-IN-16可用于炎症研究。

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NLRP3-IN-16 Chemical Structure

NLRP3-IN-16 Chemical Structure

CAS No. : 2906872-59-9

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查看 NOD-like Receptor (NLR) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-16 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-16 inhibits IL-1β release with an IC50 of 0.065 μM. NLRP3-IN-16 can be used for the research of inflammation[1].

IC50 & Target[1]

NLRP3 inflammasome

 

体外研究
(In Vitro)

NLRP3-IN-16 (化合物 12d) 抑制 IL-1β 释放,IC50 为 0.065 μM (ELISA 测定) [1]
NLRP3-IN-16 (2 μM,3 小时) 抑制小鼠腹膜巨噬细胞 (PM) 中 IL-1β (p17) 和 caspase-1 (p20) 的分泌[1]
NLRP3-IN-16 通过抑制 ASC 寡聚化来抑制 NLRP3 炎性体复合物的形成[1]
NLRP3-IN-16 在人和小鼠肝微粒体中表现出代谢稳定性 (T1/2: 223.5 min; Clint: 6.2act μL/min/mg)[1].

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

Western Blot Analysis[1]

Cell Line: Mice peritoneal macrophages(PMs)
Concentration: 2 μM
Incubation Time: 3 h
Result: Inhibited the secretion of IL-1β (p17) and caspase-1 (p20), without affecting pro-IL-1β and pro-caspase-1.
体内研究
(In Vivo)

NLRP3-IN-16 (化合物 5j) (50 mg/kg;i.p.) 在败血症小鼠模型中表现出抗炎作用[1]

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

Animal Model: LPS-induced inflammatory septic mouse model[1]
Dosage: 50 mg/kg
Administration: i.p.
Result: Decreased the release of IL-1β in mouse serum.
Relieved thickening of the alveolar wall in lung.
Animal Model: Mice[1]
Dosage: 20 or 5 mg/kg
Administration: p.o. or i.v.
Result: Pharmacokinetic profile of NLRP3-IN-15 (compound 12a).
parameter dose (mg/kg) T1/2 (h) Tmax (h) F (%)
PO 20 2.725 0.222 5.0
IV 5 2.772 0.083
分子量

419.47

Formula

C25H25NO5

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
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  • 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.

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产品名称:
NLRP3-IN-16
目录号:
HY-149123
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