通过GTP结合测得其对CXCR4活化的IC50值为10.38 ± 1.99 nM.CXCR4在多种细胞类型中广泛表达,参与新生儿发育造血作用淋巴细胞运输和归巢.另外,CXCR4是HIV的共受体,因而CXCR4的小分子拮抗剂具有治疗潜力.AMD 3465是N-吡啶基乙烯单环拉胺类CXCR4拮抗剂,抑制T细胞嗜性的使用CXCR4的HIV感染.

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

GENZ-644494

powder

Soluble in DMSO

CXCR4

Using the CCRF-CEM T-cell line expressing CXCR4 previous authors have demonstrated that AMD3465 is an antagonist of SDF-1 ligand binding, and inhibits SDF-1 mediated signaling as shown by inhibition of GTP binding, calcium flux, and inhibition of chemotaxis. AMD3465 does not inhibit chemokine-stimulated calcium flux in cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7, nor does it inhibit binding of LTB4 to its receptor, BLT1 .

AMD3465 caused leukocytosis when subcutaneously administered in mice and dogs, with peak mobilization occurring between 0.5 and 1.5 h following subcutaneous dosing in mice and with maximum peak plasma concentration of compound preceding peak mobilization in dogs, demonstrating that AMD3465 has the potential to mobilize hematopoietic stem cells. These data demonstrate the therapeutic potential for the CXCR4 antagonist AMD3465.

[1]. Rosenkilde MM, et al. Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor. J Biol Chem. 2007 Sep 14;282(37):27354-65.

[2]. Bodart V, et al. Pharmacology of AMD3465: a small molecule antagonist of the chemokine receptor CXCR4. Biochem Pharmacol. 2009 Oct 15;78(8):993-1000.