AMD 3100 octahydrochloride

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Cat.No. 3299 - AMD 3100 octahydrochloride | C28H54N8.8HCl | CAS No. 155148-31-5
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
Datasheet
Citations (9)
Reviews
Literature

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 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.

Technical Data

M. Wt 794.48
Formula C28H54N8.8HCl
Storage Desiccate 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.

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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Safety Datasheet

References

References are publications that support the products' biological activity.

Bridger et 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

Hogaboam et al (2005) The therapeutic potential in targeting CCR5 and CXCR4 receptors in infectious and allergic pulmonary disease. Pharmacol.Ther. 107 314 PMID: 16009428

Hatse et al (2002) Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4. FEBS Letts. 527 255 PMID:

Paganessi et 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


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View all Chemokine CXC Receptor Antagonists

Keywords: AMD 3100 octahydrochloride, supplier, selective, CXCR4, antagonists, Chemokine, Receptors, AMD3100, octahydrochloride, JM3100, JM, 3100, Plerixafor, Stem, Cell, Signaling, Chemokine, CXC, Receptors, Chemokine, CXC, Receptors, Tocris Bioscience

9 Citations for AMD 3100 octahydrochloride

Citations are publications that use Tocris products. Selected citations for AMD 3100 octahydrochloride include:

Chu et al (2015) CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. Neoplasia 10 e0133616 PMID: 26214690

Cavnar et al (2015) Modeling selective elimination of quiescent cancer cells from bone marrow. Cell 17 625 PMID: 26408255

Ray et al (2011) Noninvasive imaging reveals inhibition of ovarian cancer by targeting CXCL12-CXCR4. Am J Pathol 13 1152 PMID: 22241961

Laschke et al (2011) Endothelial progenitor cells contribute to the vascularization of endometriotic lesions. Development 178 442 PMID: 21224081

Beck et al (2014) CXCR4 and a cell-extrinsic mechanism control immature B lymphocyte egress from bone marrow. J Exp Med 211 2567 PMID: 25403444

Mycko et al (2014) Brain glycolipids suppress T helper cells and inhibit autoimmune demyelination. J Neurosci 34 8646 PMID: 24948818

Farkas et al (2014) CXCR4 inhibition ameliorates severe obliterative pulmonary hypertension and accumulation of C-kit+ cells in rats. PLoS One 9 e89810 PMID: 24587052

Zhang et al (2013) Selection of bone metastasis seeds by mesenchymal signals in the primary tumor stroma. Neoplasia 154 1060 PMID: 23993096

Chigaev et al (2011) Discovery of very late antigen-4 (VLA-4, alpha4beta1 integrin) allosteric antagonists. J Biol Chem 286 5455 PMID: 21131351


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