2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. NLRP3-IN-14

NLRP3-IN-14 是一种有效的、选择性的 NLRP3 炎症小体抑制剂 (KD: 5.87 μM)。NLRP3-IN-14 抑制 IL-1β 释放，IC50 为 0.131 μM。NLRP3-IN-14可用于炎症研究。

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NLRP3-IN-14 Chemical Structure

NLRP3-IN-14 Chemical Structure

CAS No. : 2767369-80-0

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NLRP3-IN-14 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation[1].

IC50 & Target[1]

NLRP3 inflammasome

5.87 μM (Kd)

体外研究
(In Vitro)

NLRP3-IN-14 (化合物 5j) 抑制 IL-1β 释放，IC50 为 0.131 μM (ELISA 测定) [1]。
NLRP3-IN-14 (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-14 通过抑制 ASC 寡聚化来抑制 NLRP3 炎性体复合物的形成[1]。
NLRP3-IN-14 (10 μM，5 小时) 随着温度升高抑制蛋白质 NLRP3 的降解[1]。
NLRP3-IN-14 在人和小鼠肝微粒体中表现出代谢稳定性 (T1/2: 866.3 min; Clint: 1.6 μL/min/mg)[1].

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

NLRP3-IN-14 相关抗体:

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-14 (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-14 (compound 5j).
parameter dose (mg/kg) T1/2 (h) Tmax (h) F (%)
PO 20 9.225 0.389 3.0
IV 5 5.028 0.083
分子量

444.52

Formula

C27H28N2O4
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-14 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-142767369-80-0NOD-like Receptor (NLR)InflammasomeIL-1βinflammationperitoneal macrophageseptic mouseLPSInhibitorinhibitorinhibit

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目录号：
HY-149121
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