2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. FABP Interleukin Related
  4. FABP4/5-IN-6

FABP4/5-IN-6 是一种口服有效的强效 FABP4/5 抑制剂 (Ki = 0.41/2.53 μM)，对 FABP3 的选择性较低 (Ki = 59.72 μM)。FABP4/5-IN-6 可抑制 Lipopolysaccharides (HY-D1056) (LPS) 诱导的 THP-1 巨噬细胞中 MCP-1 和 IL-6 的分泌。FABP4/5-IN-6 具有显著的抗炎作用，并能减轻 LPS 诱导的肝损伤。FABP4/5-IN-6 对 hERG 通道的抑制作用较弱 (LD50 > 2000 mg/kg)。FABP4/5-IN-6 可用于炎症相关疾病的研究。

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FABP4/5-IN-6

FABP4/5-IN-6 Chemical Structure

CAS No. : 2975215-64-4

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FABP4/5-IN-6 相关抗体

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查看 Interleukin Related 亚型特异性产品:

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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 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FABP4/5-IN-6 is an orally active, potent FABP4/5 inhibitor (Ki = 0.41/2.53 μM), showing low selectivity over FABP3 (Ki = 59.72 μM). FABP4/5-IN-6 inhibits the secretion of MCP-1 and IL-6 in Lipopolysaccharides (HY-D1056) (LPS)-induced THP-1 macrophage. FABP4/5-IN-6 exhibits significant anti-inflammatory effects and attenuates LPS-induced liver injury. FABP4/5-IN-6 has low hERG inhibition (LD50 > 2000 mg/kg). FABP4/5-IN-6 can be used for the study of Inflammation-related diseases[1].

体外研究
(In Vitro)

FABP4/5-IN-6 (Compound Y18) (80 μM, 24 h) shows no significant cytotoxicity to THP-1 cells, and cell viability is unaffected[1].
FABP4/5-IN-6 (5-25 μM, 24 h) significantly inhibits LPS-induced secretion of MCP-1 and IL-6 in THP-1 macrophage cells, with the inhibitory effect showing a dose-dependent effect[1].

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

FABP4/5-IN-6 相关抗体:

ELISA Assay[1]

Cell Line: LPS-induced THP-1 macrophage cells
Concentration: 5 μM, 10 μM, 25 μM
Incubation Time: Incubate 18 hours, then stimulate with LPS (100 ng/mL) for 6 hours
Result: Significantly reduced the secretion of MCP-1 and IL-6.
体内研究
(In Vivo)

FABP4/5-IN-6 (Compound Y18) (50 mg/kg，口服，每日一次，连续4天) 在小鼠体内表现出显著的抗炎和保护作用。它能有效减轻 LPS 诱导的肝损伤，抑制全身和局部肝脏炎症反应，并改善肝脾的病理损伤[1]。

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

Animal Model: Seven-week-old male C57BL/6 mice were used to develop an acute inflammation model induced by LPS[1].
Dosage: 50 mg/kg
Administration: P.o., once daily for 4 days, LPS was injected 30 minutes after the last dose
Result: Body weight remained unchanged.
Significantly reduced serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels.
Significantly inhibited LPS-induced MCP-1 elevation.
Exhibited a trend toward reducing serum IL-6 and TNF-α levels.
Reduced inflammatory cell infiltration and alleviated pathological changes in the spleen.
Significantly inhibited the LPS-induced upregulation of liver MCP-1 and CD11b (macrophage marker) gene expression, and showed an inhibitory trend on IL-6 and TNF-α gene expression.
分子量

420.26

Formula

C21H16Cl2FNO3
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

FABP4/5-IN-6 相关分类

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  • 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:

FABP4/5-IN-62975215-64-4FABPInterleukin RelatedFatty acid-binding proteinILFABP4FABP5Anti-InflammatoryLPS-Induced Liver InjuryInhibitorinhibitorinhibit

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