Home Immunology & Inflammation CCR antagonist Adaptavir (DAPTA)

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Adaptavir (DAPTA) CCR antagonist

Cat.No.S8501

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) CCR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 856.88

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 856.88 Formula

C35H56N10O15

 Storage (From the date of receipt)
CAS No. 106362-34-9 Download SDF Download SDF Storage of Stock Solutions

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

Solubility

In vitro
Batch:

Water : 100 mg/mL

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In vivo
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Mechanism of Action

Targets/IC50/Ki
gp120 Bal-CCR5 [1]
(Cell-free assay)
0.06 nM
CM235-CCR5 [1]
(Cell-free assay)
0.32 nM
In vitro
Adaptavir (DAPTA) is a non-toxic experimental antiviral entry inhibitor that 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, this compound (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. It 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 this compound 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
Following DAPTA treatment, the levels of inflammatory cytokines IL-1, IL-6, and TNFα decrease in plasma[2]. This compound also prevents the neuronal cell death associated with gpl20 and prevents gpl20-associated neural deficits in vivo[3].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00951743 Unknown status
HIV Infections
Rapid Laboratories Inc.
 July 2009 Phase 2

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