Home Immunology & Inflammation CCR antagonist Adaptavir (DAPTA) For research use only.

Adaptavir (DAPTA)

Synonyms: D-Ala-peptide T-amide, peptide T

Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5.

Adaptavir (DAPTA) Chemical Structure

Adaptavir (DAPTA) Chemical Structure

CAS: 106362-34-9

Selleck's Adaptavir (DAPTA) has been cited by 3 publications

Purity & Quality Control

Batch: S850101 Water] 100 mg/mL] false] ] ] false] ] ] false Purity: 99.34%
99.34

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Biological Activity

Description Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5.
Targets
gp120 Bal-CCR5 [1]
(Cell-free assay)		 CM235-CCR5 [1]
(Cell-free assay)
0.06 nM 0.32 nM
In vitro
In vitro DAPTA is a non-toxic experimental antiviral entry inhibitor. DAPTA potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5. In co-immunoprecipitation studies, DAPTA (1 nM) blocks formation of the gp120/sCD4 complex with CCR5. Confocal microscopic studies of direct FITC-DAPTA binding to CCR5+, but not CCR5−, cells show that CCR5 is a DAPTA receptor. DAPTA is an antagonist of CCR5-mediated chemotaxis and is most effective as an antiviral agent primarily against R5-tropic HIV-1 isolates, with reduced or absent effect for X4-tropic laboratory isolates. DAPTA does not inhibit fusion in typical assays, which use high local concentrations of virus and cells[1]. The Th2 cytokines IL-4, IL-10,and IL-13, are increased by DAPTA and induce a potent virostatic state in infected macrophages in vitro, as well as inhibit production of the proinflammatory cytokines IL-1 and TNFα, which upregulate virus expression. Thus the elevation of Th2 cytokines by DAPTA treatment would favor less macrophage viral replication[2].
Cell Research Cell lines Monocyte-derived macrophages
Concentrations 10−12 to 10−7 M
Incubation Time 7 days and 14 days
Method

MDM (Monocyte-derived macrophages) at a concentration of 1×106 cells per ml in 24-well plates are cultured for 7-14 days in growth medium (RPMI, 5% human AB serum). At the beginning of the experiment the cells are washed with serum free RPMI and are treated with peptide T (DAPTA) at the indicated concentrations, or vehicle (medium), for 1-2 h at 37 °C, 5% CO2. Cultures are washed two times to remove unabsorbed virus and cultured in growth medium containing peptide T at indicated concentrations. Supernatants from day 7 or 14 cultured MDM's are sampled. Cultures are re-fed with peptide T and 50% fresh medium after the day 7 sample. The p24 antigen determination is made using commercial kits.
In Vivo
In vivo The levels of inflammatory cytokines IL-1, IL-6, and TNFα decrease in plasma following DAPTA treatment[2]. Peptide T(DAPTA) treatment prevents the neuronal cell death associated with gpl20. DAPTA prevents gpl20-associated neural deficits in vivo[3].
Animal Research Animal Models Sprague-Dawley rats
Dosages 5 μg/100 μl
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00951743 Unknown status HIV Infections Rapid Laboratories Inc. July 2009 Phase 2

Chemical lnformation & Solubility

Molecular Weight 856.88 Formula

C35H56N10O15
CAS No. 106362-34-9 SDF Download Adaptavir (DAPTA) SDF Download Adaptavir (DAPTA) SDF
Smiles CC(C(C(=O)N)NC(=O)C(CC1=CC=C(C=C1)O)NC(=O)C(CC(=O)N)NC(=O)C(C(C)O)NC(=O)C(C(C)O)NC(=O)C(C(C)O)NC(=O)C(CO)NC(=O)C(C)N)O
Storage (From the date of receipt)

In vitro
Batch:

Water : 100 mg/mL


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