Chemical Name: 1,1'-[1,4-Phenylenebis-(methylene)]-bis-(1,4,8,11-tetraazacyclotetradecane) octahydrochloride
Biological Activity
Technical Data
Solubility
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References
Biological Activity
Highly selective CXCR4 chemokine receptor antagonist (IC50 values are 0.02 - 0.13 and > 25 μM for CXCR4 and all other chemokine receptors respectively). Switches inflammatory responses from Th4 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
water
79.45
100
Preparing Stock Solutions
The following data is based on the product molecular weight 794.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.26 mL
6.29 mL
12.59 mL
5 mM
0.25 mL
1.26 mL
2.52 mL
10 mM
0.13 mL
0.63 mL
1.26 mL
50 mM
0.03 mL
0.13 mL
0.25 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Bridgeret al (1995) 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. J.Med.Chem. 38 366 PMID: 7830280
Hogaboamet al (2005) The therapeutic potential in targeting CCR5 and CXCR4 receptors in infectious and allergic pulmonary disease. Pharmacol.Ther. 107 314 PMID: 16009428
Hatseet al (2002) Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4. FEBS Letts. 527 255 PMID:
Paganessiet al (2011) Effective mobilization of hematopoietic progenitor cells in G-CSF mobilization defective CD26-/- mice through AMD3100-induced disruption of the CXCL12-CXCR4 axis. Exp.Hematol. 39 384 PMID: 21168468