Plerixafor (AMD3100) is a bis-tetraazadecane-based, selective inhibitor of human immunodeficiency virus. It is inhibitory to the replication of various HIV-1 and HIV-2 strains in various cell lines at an EC50 of 1-10 ng/mL, about 100,000-fold lower than cytotoxic concentrations (>500 uM/mL). [1] Plerixafor shows inhibition to HIV-1(IIIB) and several clinical HIV-1 isolates at an EC50 of less than 1 ng/mL.
Plerixafor has been shown to be active in HIV strains resistant to reverse transcriptase inhibitors AZT, DDI, 3TC, aAPA, and TIBO. [2]
Plerixafor blocks HIV-1 entry and membrane fusion via the CXCR4 co-receptor, but not via CCR5. It also prevents monoclonal antibody 12G5 from binding to CXCR4. Entry into CXCR-expressing cells was strongly inhibited by Plerixafor at IC50 values of 0.01-0.1 nM. [3] Plerixafor demonstrates a specific antagonism of the interaction between chemokine SDF-1 and CXCR4, reducing severity of inflammation in CIA models. [4]
Technical information:
| Chemical Formula: | C28H54N8 | |
| CAS #: | 110078-46-1, 155148-31-5 | |
| Molecular Weight: | 502.78 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 1,1'-[1,4-Phenylenebis(methylene)]bis [1,4,8,11-tetraazacyclotetradecane] | |
| Solubility: | Up to 100 mM in water in DMSO | |
| Synonyms: | AMD3100, AMD 3100, Plerixafor, Mozobil, bicyclam JM-2987 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | De Clercq et al., Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob. Agents Chemother. 1994, 38(4), 668-674. Pubmed ID: 7913308 |
| 2. | Este et al., Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human immunodeficiency virus type 1. Antiviral Res. 1996, 29, 297-307. Pubmed ID: 8739608 |
| 3. | Donzella et al., AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor. Nature Med. 1998, 4(1), 72-77. Pubmed ID: 9427609 |
| 4. | Matthys et al., AMD3100, a potent and specific antagonist of the stromal cell-derived factor-1 chemokine receptor CXCR4, inhibits autoimmune joint inflammation in IFN-gamma receptor-deficient mice. J. Immunol. 2001, 167(8), 4686-4692. Pubmed ID: 8739608 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
