AMD 3100 octahydrochloride

Name: AMD 3100 octahydrochloride
Brand: Tocris Bioscience
SKU: 3299

Tocris Bioscience, part of Bio-Techne | Catalog # 3299

Citations (31)

COA / SDS

Highly selective CXCR4 antagonist

Key Product Details

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
Molecular Weight:	794.48

View Full Technical Details for AMD 3100 octahydrochloride

Technical Data
Citations

Biological Activity for AMD 3100 octahydrochloride

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 for AMD 3100 octahydrochloride

M. Wt	794.48
Formula	C₂₈H₅₄N₈.8HCl
Storage	Store at -20°C
CAS Number	155148-31-5
PubChem ID	65014
InChi Key	UEUPDYPUTTUXLJ-UHFFFAOYSA-N
Smiles	C1(CN3CCCNCCNCCCNCC3)=CC=C(CN2CCCNCCNCCCNCC2)C=C1.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl

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.

Solubility for AMD 3100 octahydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	79.45	100

Preparing Stock Solutions for AMD 3100 octahydrochloride

The following data is based on the product molecular weight 794.48.

Batch specific molecular weights may vary from batch to batch due to the degree 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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References for AMD 3100 octahydrochloride

References are publications that support the biological activity of the product.

Kalatskaya MD3100 Is a CXCR7 ligand with allosteric agonist properties. Mol.Pharmacol, 2009 PMID: 19255243
Wu A novel CXCR4 antagonist CX549 induces neuroprotection in stroke brain. Cell.Transplant. 2017 PMID: 27938478
Burger and Peled CXCR4 antagonists: targeting the microenvironment in leukemia and other cancers. Leukemia 2009 PMID: 18987663
Kim Chemokines and cocaine: CXCR4 receptor antagonist AMD3100 attenuates cocaine place preference and locomotor stimulation in rats. Brain Behav.Immun. 2017 PMID: 27575003
Paganessi Effective mobilization of hematopoietic progenitor cells in G-CSF mobilization defective CD26-/- mice through AMD3100-induced disruption of the CXCL12-CXCR4 axis. Exp.Hematol. 2011 PMID: 21168468
Hatse Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4. FEBS Letts. 2002 PMID: 12220670
Hogaboam The therapeutic potential in targeting CCR5 and CXCR4 receptors in infectious and allergic pulmonary disease. Pharmacol.Ther. 2005 PMID: 16009428
Bridger 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. 1995 PMID: 7830280