同义名 :	Tyrphostin 1; AG9
	CAS号 :	2826-26-8
	货号 :	A630950
	分子式 :	C11H8N2O
	纯度 :	99%+
	分子量 :	184.19
	MDL号 :	MFCD00019787
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Tyrphostin A1 (AG9) is effective in inhibiting CD40L-stimulated IL-12 production in macrophage cultures and preventing the antigen-induced generation of Th1 cells. Its application leads to a dose-dependent reduction of IL-12 p40 levels, achieving maximum inhibition (62.5%) at a 10 μM concentration. Tyrphostin A1 also obstructs the CD40L-induced translocation of NF-κB to the nucleus and diminishes the activation of the IL-12 p40 gene. Therapeutic use of A1 in vivo results in decreased generation of myelin basic protein (MBP) specific encephalitogenic T cells and attenuates experimental allergic encephalomyelitis (EAE) in SJL/J mice, highlighting its potential for therapeutic applications in autoimmunity [1]. Compared to other tyrphostins, Tyrphostin A1 is a significantly weaker inhibitor of tyrosine kinase (TK), with an IC50 greater than 1250 μM for the epidermal growth factor receptor (EGFR) kinase, indicating its utility in distinguishing TK-mediated effects from non-specific actions of tyrphostins [2].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	5.43mL 1.09mL 0.54mL	27.15mL 5.43mL 2.71mL	54.29mL 10.86mL 5.43mL

参考文献

[1]Du C, et al. Inhibition of CD40 signaling pathway by tyrphostin A1 reduces secretion of IL-12 in macrophage, Th1 cell development and experimental allergic encephalomyelitis in SJL/J mice. J Neuroimmunol. 2001 Mar 1;114(1-2):69-79. [2]Ogura T, et al. Activation of background membrane conductance by the tyrosine kinase inhibitor tyrphostin A23 and its inactive analog tyrphostin A1 in guinea pig ventricular myocytes. Jpn J Pharmacol. 2001 Nov;87(3):235-9.