DAPTA

Catalog No.S8501 Synonyms: D-Ala-peptide T-amide, peptide T

DAPTA Chemical Structure

Molecular Weight(MW): 856.88

DAPTA 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.

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Biological Activity

Description DAPTA 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

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].

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].

Protocol

Cell Research:

[4]

+ Expand
  • 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 1×10<sup>6</sup> 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.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: Saline
  • Dosages: 5 μg/100 μl
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (116.7 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 856.88
Formula

C35H56N10O15

CAS No. 106362-34-9
Storage powder
Synonyms D-Ala-peptide T-amide, peptide T

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID