Adaptavir (DAPTA)

Catalog No.S8501 Batch:S850101

Technical Data

Formula	C₃₅H₅₆N₁₀O₁₅
Molecular Weight	856.88	CAS No.	106362-34-9
Solubility (25°C)*	In vitro	Water	100 mg/mL (116.7 mM)


* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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 (from reference)

Cell Assay:^{^[4]}	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.
Animal Study:^{^[3]}	Animal Models Sprague-Dawley rats Dosages 5 μg/100 μl Administration s.c.

Cell Assay:^{^[4]}

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.

Animal Study:^{^[3]}

Animal Models
Sprague-Dawley rats
Dosages
5 μg/100 μl
Administration
s.c.

References

[4] Ruff MR, et al. Antiviral Res. 2001, 52(1):63-75.

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

Cancer associated fibroblast-derived CCL5 promotes hepatocellular carcinoma metastasis through activating HIF1α/ZEB1 axis [ Cell Death Dis, 2022, 13(5):478]	PubMed: 35589690
Chemokine CCL5 promotes robust optic nerve regeneration and mediates many of the effects of CNTF gene therapy [ Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118]	PubMed: 33627402
Cholesterol impacts chemokine CCR5 receptor ligand-binding activity [ FEBS J, 2020, 287(11):2367-2385]	PubMed: 31738467

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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