2. Immunology/Inflammation
  3. NOD-like Receptor (NLR) Interleukin Related
  4. NLRP3-IN-42

NLRP3-IN-42 (compound H28) 是一种有效的 NLRP3 抑制剂，其 KD 值为 1.15 µM。NLRP3-IN-42 可降低 LPS (HY-D1056) 诱导的 cleaved-caspase-1 (p20) 的蛋白表达。NLRP3-IN-42 可选择性抑制 IL-1β 释放。

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NLRP3-IN-42 Chemical Structure

NLRP3-IN-42 Chemical Structure

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NLRP3-IN-42 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-42 (compound H28) is a potent NLRP3 inhibitor with an KD value of 1.15 µM. NLRP3-IN-42 decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20). NLRP3-IN-42 selectively inhibits IL-1β release[1].

IC50 & Target[1]

NLRP3

1.15 μM (Kd)

IL-1β

 

体外研究
(In Vitro)

NLRP3-IN-42 (compound H28) (0-30 µM) 以剂量依赖性方式降低 LPS (HY-D1056) 诱导的 cleaved-caspase-1 (p20) 的表达[1]。
NLRP3-IN-42 可以稳定地结合 NLRP3 NACHT 结构域的 ADP 活性位点[1]。

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

NLRP3-IN-42 相关抗体:

Western Blot Analysis[1]

Cell Line: J774A.1 cells
Concentration: 0, 3, 10, 30 µM
Incubation Time: 2.5 h + 30 min
Result: Decreased the LPS (1 μg/mL) induced protein expression of cleaved-caspase-1 (p20) in culture supernatants (SN) and whole cell lysates (WCL) in a dose-dependent manner.
体内研究
(In Vivo)

NLRP3-IN-42 (10 mg/kg; i.p.) 通过抑制 NLRP3 炎症小体选择性抑制 IL-1β 释放，而不会显著影响炎症因子 TNF-α[1]。
药代动力学分析 (ICR mice)[1].

PK parameters H28
Administered dose (mg/kg) iv at 2.5 mg/kg
AUC0-∞ (h*ng/mL) 1189 ± 137
t1/2 (h) 1.69 ± 0.38
CL (mL/h/kg) 35.36 ± 4.12
Cmax (ng/mL) 2987 ± 281

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

Animal Model: 4-8 weeks, Male C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: I.p; 1 h before injection of LPS (35 mg/kg, ip) for 2.5 h
Result: Significantly inhibited IL-1β production in the treatment mice. It is noteworthy that the treatment with these compounds do not result in significant inhibition of TNF-α levels.
分子量

572.66

Formula

C29H27F3N2O3S2
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-42 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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-42NOD-like Receptor (NLR)Interleukin RelatedILcleaved-caspase-1 (p20)J774A.1 cellsIL-1βLPSTNF-αInhibitorinhibitorinhibit

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目录号：
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