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%
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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
(Cell-free assay)
0.06 nM
CM235-CCR5
(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. 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.
In vivo
Following DAPTA treatment, the levels of inflammatory cytokines IL-1, IL-6, and TNFα decrease in plasma. This compound also prevents the neuronal cell death associated with gpl20 and prevents gpl20-associated neural deficits in vivo.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11530189/

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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