生物活性

This compound is a known, potent initiator of the proinflammatory response and induces proinflammatory cytokines in several cell types. Many of the cell signals induced by gram-negative bacteria are attributed to LPS and have been observed to also activate TNF receptor signaling pathways. The major receptor that transduces the LPS signal has been recognized as a member of the Toll-like receptor family. At least 10 members of the family have been identified to date and TLR4 appears to be the main LPS receptor although coreceptors are most likely involved. Studies note that in HMEC (human microvascular endothelial cells) cell lines, LPS activates apoptosis pathways via both NF-κB and JNK through TRAF6. Also reported that NF-κB inhibition does not potentiate LPS-induced death in HMEC cells yet will sensitize these cell to TNF-induced death. Additional studies using HMEC cell lines report that following LPS stimulation, TRAF6 also transmits an important endothelial cell survival signal in a situation of complete NF-κB blockade which may indicate that TRAF6 signals an NF-κB–independent antiapoptotic pathway in endothelial cells exposed to LPS.

体外研究

体内研究

激酶实验

细胞实验

1 mg/ 1 mL再逐步稀释

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Zhang, F.X., et al. 1999. J. Biol. Chem. 274: 7611-7614. PMID: 10075645
[2] Hull, C., et al. 2002. J. Immunol. 169: 2611-2618. PMID: 12193732
[3] Raschi, E., et al. 2003. Blood. 101: 3495-3500. PMID: 12531807
[4] Hattori, S., et al. 1995. Biochem. Mol. Biol. Int. 35: 177-183. PMID: 7537570
[5] Mayeux, P.R., et al. 1995. Biochem. Pharmacol. 49: 115-118. PMID: 7530953

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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