Biochem/physiol Actions

Reversible: yes

General 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)