Plerixafor (AMD3100) 110078-46-1

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Molecular Weight:

502.78 Plerixafor is a Chemokine Receptor Antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Biological Activity

Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of
651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated
calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM
and 51 nM, respectively.


Plerixafor does not inhibit calcium flux
against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when
stimulated with their cognate ligands, nor does Plerixafor inhibit
receptor binding of LTB4. Plerixafor does not, on its own, induce a
calcium flux in the CCRF–CEM cells, which express multiple GPCRs
including CXCR4, CCR4 and CCR7.


A single topical application of Plerixafor promotes wound healing in
diabetic mice by increasing cytokine production, mobilizing bone marrow
EPCs, and enhancing the activity of fibroblasts and
monocytes/macrophages, thereby increasing both Angiogenesis and
vasculogenesis.


Cohorts of mice are administered with
PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor
on the 5th day. The number and size of the colonies are highest in IGF1
plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated
groups, in combination with Plerixafor.

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Product Categories : GPCR & G Protein > CXCR Inhibitor