AMD 3100 octahydrochloride

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3299/10
3299/50
AMD 3100 octahydrochloride | CAS No. 155148-31-5 | Chemokine Receptor Antagonists
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Description: Highly selective CXCR4 antagonist
Alternative Names: JM 3100,Plerixafor

Chemical Name: 1,1'-[1,4-Phenylenebis-(methylene)]-bis-(1,4,8,11-tetraazacyclotetradecane) octahydrochloride

Product Details
Citations (16)
Supplemental Products
Reviews

Biological Activity

AMD 3100 octahydrochloride is a highly selective CXCR4 chemokine receptor antagonist (IC50 values are 0.02 - 0.13 and > 25 μM for CXCR4 and most other chemokine receptors, respectively). Also CXCR7 allosteric agonist. Switches inflammatory responses from Th2 to Th1 type and reduces airway hyperresponsiveness in a mouse model of asthma. Potently inhibits HIV-1 and HIV-2 replication in vitro (EC50 = 4 - 35 nM) and mobilizes hematopoietic stem cells in vivo. Attenuates cocaine place preference and locomotor stimulation in rats. Attenuates microglial activation neurological function after ischemic stroke in mice. Inhibits tumor cell migration and proliferation in vitro and in vivo in a range of cancers.

Technical Data

M.Wt:
794.48
Formula:
C28H54N8.8HCl
Solubility:
Soluble to 100 mM in water
Storage:
Store at -20°C
CAS No:
155148-31-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Brain glycolipids suppress T helper cells and inhibit autoimmune demyelination.
    Mycko M, Sliwinska B, Cichalewska M, Cwiklinska H, Raine C, Selmaj K
    J Neurosci, 2014;34(25):8646-58.
  2. I-bodies: human single domain antibodies that antagonize chemokine receptor CXCR4
    K Griffiths, O Dolezal, B Cao, SK Nilsson, HB See, KD Pfleger, M Roche, PR Gorry, A Pow, K Viduka, K Lim, BG Lu, DH Chang, TA Murray-Rus, M Kvansakul, MA Perugini, C Dogovski, M Doerflinge, Y Zhang, K Parisi, JL Casey, SD Nuttall, M Foley
    J Biol Chem, 2016;0(0):.
  3. CXCR4 and a cell-extrinsic mechanism control immature B lymphocyte egress from bone marrow.
    Beck T, Gomes A, Cyster J, Pereira J
    J Exp Med, 2014;211(13):2567-81.
  4. SDF-1alpha is a novel autocrine activator of platelets operating through its receptor CXCR4.
    Walsh T, Harper M, Poole A
    Cell Signal, 2015;27(1):37-46.
  5. Hematopoietic stem cell mobilizing agents G-CSF, cyclophosphamide or AMD3100 have distinct mechanisms of action on bone marrow HSC niches and bone formation.
    Winkler IG, Pettit AR, Raggatt LJ, Jacobsen RN, Forristal CE, Barbier V, Nowlan B, Cisterne A, Bendall LJ, Sims NA, Levesque JP
    Leukemia, 2012;26(7):1594-601.
  6. Affinity biosensors using recombinant native membrane proteins displayed on exosomes: application to botulinum neurotoxin B receptor
    R Desplantes, C Lévêque, B Muller, M Lotierzo, G Ferracci, M Popoff, M Seagar, R Mamoun, O El Far
    Sci Rep, 2017;7(1):1032.
  7. Secondary lymphoid organ homing phenotype of human myeloid dendritic cells disrupted by an intracellular oral pathogen.
    Miles, Brodie, Zakhary, Ibrahim, El-Awady, Ahmed, Scisci, Elizabet, Carrion, Julio, O'Neill, John C, Rawlings, Aaron, Stern, J Kobi, Susin, Cristian, Cutler, Christop
    Infect Immun, 2014;82(1):101-11.
  8. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibits HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker.
    Bridger et al.
    J.Med.Chem., 1995;38:366
  9. The therapeutic potential in targeting CCR5 and CXCR4 receptors in infectious and allergic pulmonary disease.
    Hogaboam et al.
    Pharmacol.Ther., 2005;107:314
  10. Effective mobilization of hematopoietic progenitor cells in G-CSF mobilization defective CD26-/- mice through AMD3100-induced disruption of the CXCL12-CXCR4 axis.
    Paganessi et al.
    Exp.Hematol., 2011;39:384
  11. Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4.
    Hatse et al.
    FEBS Letts., 2002;527:255
  12. Chemokines and cocaine: CXCR4 receptor antagonist AMD3100 attenuates cocaine place preference and locomotor stimulation in rats.
    Kim et al.
    Brain Behav.Immun., 2017;62:30
  13. A novel CXCR4 antagonist CX549 induces neuroprotection in stroke brain.
    Wu et al.
    Cell.Transplant., 2017;26:571
  14. CXCR4 antagonists: targeting the microenvironment in leukemia and other cancers.
    Burger and Peled et al.
    Leukemia, 2009;23:43
  15. MD3100 Is a CXCR7 ligand with allosteric agonist properties.
    Kalatskaya et al.
    Mol.Pharmacol,, 2009;75:1240

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Citations for AMD 3100 octahydrochloride

The citations listed below are publications that use Tocris products. Selected citations for AMD 3100 octahydrochloride include:

16 Citations: Showing 1 - 10

  1. Oral Pathobiont Activates Anti-Apoptotic Pathway, Promoting both Immune Suppression and Oncogenic Cell Proliferation.
    Authors: Arjunan Et al.
    Sci Rep  2018;8:16607
  2. Anti-fibrotic effects of CXCR4-targeting i-body AD-114 in preclinical models of pulmonary fibrosis.
    Authors: Griffiths
    Sci Rep  2018;8(1):3212
  3. Circadian Expression of Migratory Factors Establishes Lineage-Specific Signatures that Guide the Homing of Leukocyte Subsets to Tissues.
    Authors: He Et al.
    Immunity  2018;49:1175
  4. CXCR4-expressing Mist1 + progenitors in the gastric antrum contribute to gastric cancer development.
    Authors: Sakitani
    Oncotarget  2017;8(67):111012
  5. Agarose Spot as a Comparative Method for in situ Analysis of Simultaneous Chemotactic Responses to Multiple Chemokines.
    Authors: Ahmed Et al.
    Sci Rep  2017;7:1075
  6. Modeling selective elimination of quiescent cancer cells from bone marrow.
    Authors: Cavnar Et al.
    Cell  2015;17:625
  7. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis.
    Authors: Chu Et al.
    Neoplasia  2015;10:e0133616
  8. Macrophage Migration Inhibitory Factor Mediates PAR-Induced Bladder Pain.
    Authors: Kouzoukas Et al.
    PLoS One  2015;10:e0127628
  9. CXCR4 inhibition ameliorates severe obliterative pulmonary hypertension and accumulation of C-kit+ cells in rats.
    Authors: Farkas Et al.
    PLoS One  2014;9:e89810
  10. Brain glycolipids suppress T helper cells and inhibit autoimmune demyelination.
    Authors: Mycko Et al.
    J Neurosci  2014;34:8646

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