CXCR4 抑制剂 Plerixafor (AMD3100) 是一种有效的 CXCL12 介导的趋化性抑制剂 (IC 50 ，5.7 nM)，效力略优于其对 CXCR4 的亲和力。 Plerixafor 干扰 CXCR4 与其天然配体 SDF-1 (CXCL12) 的相互作用。

Plerixafor, sold under the brand name Mozobil, is an immunostimulant used to mobilize hematopoietic stem cells in cancer patients into the bloodstream. The stem cells are then extracted from the blood and transplanted back to the patient. The drug was developed by AnorMED, which was subsequently bought by Genzyme.

AMD3100 (plerixafor), a CXCR4 antagonist, has opened a variety of avenues for potential therapeutic approaches in different refractory diseases. The CXCL12/CXCR4 axis and its signaling pathways are involved in diverse disorders including HIV-1 infection, tumor development, non-Hodgkin lymphoma, mult …

Plerixafor (AMD3100, JM 3100, SID791)是一种趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导的趋化性，无细胞试验中IC50分别为44 nM和5.7 nM。 Plerixafor 可抑制human immunodeficiency virus (HIV)复制。

Jan 18, 2014 · amd3100是一种人工合成的大环类sdf1受体cxcr4特异性拮抗剂，amd3100可有效地与cxcr4结合阻断sdf1与cxcr4之间的信号转导但不能对cxcr4产生激动作用，这是amd3100发挥生物学作用的基础。

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Jul 1, 2003 · The discovery and development of the bicyclam AMD3100 — a chemokine receptor antagonist — has highlighted the therapeutic potential of such compounds in HIV infection, inflammatory diseases ...

AMD3100, a specific inhibitor of CXCR4, one of the key molecules that tethers hematopoietic stem cells to the bone marrow microenvironment, is a promising new agent currently in clinical development for autologous and allogeneic stem cell mobilization.

AMD3100 was shown to specifically antagonize CXCR4, and thus to block the entry of the T-lymphotropic HIV strains (6–8). AMD3100 appears to be a highly specific inhibitor of CXCR4 : it only blocks, as measured by the Ca ++ flux, the signal pathway from CXCR4 (Figure 1B) and not that of any other receptor for either CXC- or C–C-chemokines .

AMD3100 (plerixafor, Mozobil®) was first identified as an anti-HIV agent specifically active against the T4-lymphotropic HIV strains, as it selectively blocked the CXCR4 receptor.