同义名 :	Takeda 779
	CAS号 :	229005-80-5
	货号 :	A734428
	分子式 :	C33H39ClN2O2
	纯度 :	99%+
	分子量 :	531.13
	MDL号 :	MFCD05662319
	存储条件：	Pure form Inert atmosphere, 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

TAK-779 demonstrates potent and selective nonpeptide antagonism against CCR5, exhibiting a Ki of 1.1 nM. It effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 values of 1.2 nM and 5.7 nM, correspondingly, in MAGI-CCR5 cells. Although less potent, TAK-779 partially impedes the binding of [125I]-monocyte chemotactic protein 1 to CCR2b in CHO/CCR2b cells, with an IC50 of 27 nM. Moreover, it entirely blocks the binding of [125I]-RANTES to CHO/CCR5 cells, with an IC50 of 1.4 nM. At a concentration of 20 nM, TAK-779 selectively hampers CCR5-mediated Ca2+-signaling. Notably, TAK-779 exhibits no inhibitory effect on X4 HIV-1 strains. TAK-779 functions as a CXCR3 antagonist, effectively impeding the migration of T cells while leaving T cell proliferation unaffected.

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.88mL 0.38mL 0.19mL	9.41mL 1.88mL 0.94mL	18.83mL 3.77mL 1.88mL

参考文献

[1]Baba M, et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5698-703. [2]Takama Y, et al. Effects of a calcineurin inhibitor, FK506, and a CCR5/CXCR3 antagonist, TAK-779, in a rat small intestinal transplantation model. Transpl Immunol. 2011 Jul;25(1):49-55. [3]Ni J, et al. The chemokine receptor antagonist, TAK-779, decreased experimental autoimmune encephalomyelitis by reducing inflammatory cell migration into the central nervous system, without affecting T cell function. Br J Pharmacol. 2009 Dec;158(8):2046-5