1. Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease NF-κB
  2. NOD-like Receptor (NLR) Pyroptosis Caspase Interleukin Related Reactive Oxygen Species (ROS)
  3. M464

M464 是一种非甾体类抗炎化合物,是一种强效且口服有效的 NLRP3 炎症小体抑制剂。M464 通过抑制 ASC 寡聚化和减少 ROS 的产生,抑制细胞焦亡 (pyroptosis),并阻断下游 Caspase-1 的表达和 IL-1β 的释放。M464 对小鼠急性肺损伤和肝损伤具有保护作用。M464 可用于 NLRP3 相关炎症性疾病的研究。

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M464

M464 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

M464, a non-steroidal anti-inflammatory compound, is a potent and orally active NLRP3 inflammasome inhibitor. M464 inhibits pyroptosis and hinders the activation of downstream Caspase-1 expression and the release of IL-1β by impeding ASC oligomerisation and curtailing ROS production. M464 exhibits protective effects against acute lung and liver injury in mice. M464 can be used for the research of NLRP3-related inflammatory diseases[1].

IC50 & Target[1]

NLRP3 inflammasome

 

体外研究
(In Vitro)

M464 (3-12 μM) 抑制与 NLRP3 炎症小体激活相关的标志蛋白 (IL-1β 和 Caspase-1) 的表达,并抑制 J774A.1 和 THP-1 细胞中细胞内 ROS 的产生和 ASC 寡聚体的形成[1]
M464 (3-12 μM;1 小时) 可抑制 J774A.1 和 THP-1 细胞中由 NLRP3 炎症小体刺激物触发的巨噬细胞焦亡[1]

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

体内研究
(In Vivo)

M464 (15, 30, 60 mg/kg;灌胃;于 LPS 注射前 1 小时单次给药) 通过抑制 NLRP3 炎症小体活化来减轻 LPS (HY-D1056) 诱导的小鼠急性肺损伤[1]
M464 (15, 30, 60 mg/kg;灌胃;于 LPS 注射前 1 小时单次给药) 通过抑制 NLRP3 炎症小体活化来减轻 LPS 和 D-GalN 诱导的小鼠急性肝损伤[1]

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

Animal Model: Male KM mice (42-56 days old) intraperitoneally injected with LPS (10 mg/kg)[1]
Dosage: 15, 30, 60 mg/kg
Administration: i.g.; single dose; 1 hour before LPS injection
Result: Dose-dependently reduced the pathological scores of lung injury.
Significantly improved the lung tissue damage in mice.
Inhibited the lung wet/dry (W/D) weight ratio and significantly improved pulmonary edema in mice.
Significantly reduced the levels of mature IL-1β and Caspase-1.
Animal Model: Male KM mice (42-56 days old) intraperitoneally injected with LPS (50 μg/kg) and D-GalN (800 mg/kg)[1]
Dosage: 15, 30, 60 mg/kg
Administration: i.g.; 1 hour before LPS injection
Result: Reversed the LPS and D-GalN induced increase of the liver-to-body weight ratio.
Markedly attenuated LPS/D-GalN-induced liver injury in mice.
Exhibited dose-dependent suppression of serum levels of AST and ALT.
Effectively suppressed the mature IL-1β release and Caspase-1 production in a dose-dependent manner.
Effectively reversed the LPS/D-GalN-induced reduction in SOD content and increase in MDA level.
分子量

464.66

Formula

C23H28O4S3

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
  • 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)

质量   浓度   体积   分子量 *
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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)
× = ×
C1   V1   C2   V2
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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M464
目录号:
HY-179494
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