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Description
Overview
A cell-permeable macrocyle cyclotriazadisulfonamide derivative compound that inhibits HIV replication (IC50 = 300 nM to 3.3 µM) and entry into cells by blocking co-translational translocation of nascent CD4 across endoplasmic reticulum membranes. Its action appears to be highly selective in reducing the expression of human CD4 and it does not affect the level of any other cell surface marker studied. Does not affect CD4 mRNA levels in cells. Shown to be effective against HIV-1 subtypes A to H, AE, and O and human herpesvirus 7 (HHV-7; IC50, 300 nM to 1.5 µM) in T-cell lines and PBMCs. Also reported to block X4 HIV-1 NL4.3 and R5 SIVmac251 laboratory strains infection in human T cells. Can act synergistically with cellulose acetate phthalate (CAP) and other anti-HIV drugs to inhibit HIV-1 and SIV infections.
Catalogue Number
534337
Brand Family
Calbiochem®
Synonyms
1-Benzyl-7-methylene-5,9-ditosyl-5,9-diaza-azoniacyclododecan-1-ium chloride, CD4 Inhibitor, CADA
References
References
Vermeire, K., et al. 2008. Curr. HIV Res.6, 246. Bell, T. W., et al. 2006. J. Med. Chem.49, 1291. Vermeire, K., et al. 2004. AIDS.18, 2115. Vermeire, K., et al. 2002. Virology.302, 342.
Vermeire, K., et al. 2008. Curr. HIV Res.6, 246. Bell, T. W., et al. 2006. J. Med. Chem.49, 1291. Vermeire, K., et al. 2004. AIDS.18, 2115. Vermeire, K., et al. 2002. Virology.302, 342.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
28-July-2017 JSW
Synonyms
1-Benzyl-7-methylene-5,9-ditosyl-5,9-diaza-azoniacyclododecan-1-ium chloride, CD4 Inhibitor, CADA
Description
A cell-permeable macrocyle cyclotriazadisulfonamide derivative compound that inhibits HIV replication (IC50 = 300 nM to 3.3 µM) and entry into cells by blocking co-translational translocation of nascent CD4 across endoplasmic reticulum membranes. Its action appears to be highly selective in reducing the expression of human CD4 and it does not affect the level of any other cell surface marker studied. Does not affect CD4 mRNA levels in cells. Shown to be effective against HIV-1 subtypes A to H, AE, and O and human herpesvirus 7 (HHV-7; IC50, 300 nM to 1.5 µM) in T-cell lines and PBMCs. Also reported to block X4 HIV-1 NL4.3 and R5 SIVmac251 laboratory strains infection in human T cells. Can act synergistically with cellulose acetate phthalate (CAP) and other anti-HIV drugs to inhibit HIV-1 and SIV infections.
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₃₁H₃₉N₃O₄S₂·HCl
Purity
≥98% by HPLC
Solubility
DMSO (10 mg/ml). Insoluble in water.
Storage
Protect from light
-20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Vermeire, K., et al. 2008. Curr. HIV Res.6, 246. Bell, T. W., et al. 2006. J. Med. Chem.49, 1291. Vermeire, K., et al. 2004. AIDS.18, 2115. Vermeire, K., et al. 2002. Virology.302, 342.