1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. M62812 free base

M62812 (free base) 是一种 toll 样受体 4 (TLR4) 信号转导抑制剂。M62812 可抑制内皮细胞和白细胞活化,防止小鼠发生致死性感染性休克。M62812 可用于脓毒症的研究。

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M62812 free base Chemical Structure

M62812 free base Chemical Structure

CAS No. : 613262-61-6

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生物活性

M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
7 μM
Compound: 23
Antagonist activity at human TLR4 expressed in HE293 cells by ELAM1-luciferase reporter gene assay
Antagonist activity at human TLR4 expressed in HE293 cells by ELAM1-luciferase reporter gene assay
[PMID: 18828583]
体外研究
(In Vitro)

M62812 (0-10 μg/ml) 抑制人血管内皮细胞和外周单核细胞中 LPS 诱导的炎性细胞因子、粘附分子和促凝活性的上调[1]

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

体内研究
(In Vivo)

M62812 (i.v.; 10-20 mg/kg; single) 在小鼠 d-半乳糖胺致敏内毒素休克模型中保护小鼠免受致死并降低炎症和凝血参数[1]
M62812 (20 mg/kg/day) 在小鼠盲肠结扎和穿刺模型中防止小鼠死亡[1]

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

Animal Model: D-galactosamine-sensitized endotoxin shock mouse model[1]
Dosage: 10-20 mg/kg
Administration: Single intravenous administration
Result: Suppressed LPS-induced leukocyte and endothelial cell activation in vivo.
Prolonged survival in a d-galactosamine-sensitized endotoxin shock mouse model.
Animal Model: A cecal ligation and puncture mouse model[1]
Dosage: 20 mg/kg
Administration: Intravenous administration; Everyday
Result: Reduced mortality in a murine cecal ligation and puncture model.
分子量

257.31

Formula

C13H11N3OS

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:
M62812 free base
目录号:
HY-103639
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