| Description | DAPTA (Adaptavir) is an inhibitor of CCR5, shows potent anti-HIV activities. |
| In vitro | D-Ala-peptide T-amide (DAPTA), or Peptide T, named for its high threonine content (ASTTTNYT), is a synthetic peptide comprised of eight amino acids (185-192) of the gp120 V2 region and functions as a viral entry inhibitor by targeting selectively CCR5.?The anti-HIV-1 activity of DAPTA was evaluated in M/M infected with R5 HIV-1 strains.?DAPTA at 10(-9) M inhibited HIV-1 replication in M/M by > 90%.?PCR analysis of viral cDNA in M/M showed that DAPTA blocks HIV entry and in this way prevents HIV-1 infection.?Moreover, DAPTA acts as a strong inhibitor and was more active than the non-peptidic CCR5 antagonist TAK-779 in inhibiting apoptosis (mediated by RS HIV-1 strains produced and released by infected M/M) on a neuroblastoma cell line[1] |
| Target activity | Gp120CM CM235/sCD4-CCR5:0.32 nM (IC50, in Cf2Th/synR5 cells), Gp120 BaL/sCD4-CCR5:55 pM (IC50, in Cf2Th/synR5 cells) |
| Synonyms | DAPTA(TFA), D-Ala-peptide T-amide, Adaptavir |
| molecular weight | 856.88 |
| Molecular formula | C35H56N10O15 |
| CAS | 106362-34-9 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10mM |
| References | 1. Pollicita M , Ruff M R , Pert C B , et al. Profound Anti-HIV-1 Activity of DAPTA in Monocytes/macrophages and Inhibition of CCR5-mediated Apoptosis in Neuronal Cells[J]. Antiviral Chemistry and Chemotherapy, 2007, 18(5):285-295. 2. Michael R. Ruff, Maria Polianova, Quan-en Yang, Gifford S. Leoung, Francis W. Ruscetti, Candace B. Pert. Update on D-Ala-Peptide T-Amide (DAPTA): A Viral Entry Inhibitor that Blocks CCR5 Chemokine Receptors[J]. Current HIV Research, 2003, 1(1):p.51-67. |