DAPTA

SKU: orb1299650

Description

DAPTA (Adaptavir) is a small molecule CCR5 antagonist with demonstrated anti-HIV activity. It is a research tool for studying viral entry mechanisms and has been utilized in both in vitro assays and in vivo animal models of HIV infection.

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 106362-34-9
• MW: 856.88
• Purity: >99.99% (May vary between batches)
• Formula: C₃₅H₅₆N₁₀O₁₅
• SMILES: C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](C)N)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)C(N)=O
• Target: CCR,HIV Protease
• Solubility: DMSO:10 mM

Bioactivity

• Target IC50:
  Gp120CM CM235/sCD4-CCR5:0.32 nM (IC50, in Cf2Th/synR5 cells)|Gp120 BaL/sCD4-CCR5:55 pM (IC50, in Cf2Th/synR5 cells)
• In Vitro:
  D-Ala-peptide T-amide (DAPTA), or Peptide T, named for its high threonine content (ASTTTNYT), is a synthetic peptide comprised of eight amino acids (185-192) of the gp120 V2 region and functions as a viral entry inhibitor by targeting selectively CCR5. The anti-HIV-1 activity of DAPTA was evaluated in M/M infected with R5 HIV-1 strains. DAPTA at 10(-9) M inhibited HIV-1 replication in M/M by > 90%. PCR analysis of viral cDNA in M/M showed that DAPTA blocks HIV entry and in this way prevents HIV-1 infection. Moreover, DAPTA acts as a strong inhibitor and was more active than the non-peptidic CCR5 antagonist TAK-779 in inhibiting apoptosis (mediated by RS HIV-1 strains produced and released by infected M/M) on a neuroblastoma cell line

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HIV Protease, HIV, HIVProtease, CCR, CCR5, Adaptavir, CC chemokine receptor, D-Ala-peptide T-amide, DAPTA

Compound Identifiers

PubChem CID

184644