DAPTA is a potent and selective CCR5 antagonist
CAS Number: 106362-34-9
Molecular Weight: 856.88
Chemical Name: L-Threoninamide, D-alanyl-L-seryl-L-threonyl-L-threonyl-L-threonyl-L-asparaginyl-L-tyrosyl-
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: H2O : 50 mg/mL (58.35 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
The levels of inflammatory cytokines IL-1, IL-6, and TNFα decrease in plasma following DAPTA treatment. Peptide T(DAPTA) treatment prevents the neuronal cell death associated with gpl20. DAPTA prevents gpl20-associated neural deficits in vivo.
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- Ruff MR, et al. Curr HIV Res. 2003, 1(1):51-67.
- Hill JM, et al. Brain Res. 1993, 603(2):222-33.
- Ruff MR, et al. Antiviral Res. 2001, 52(1):63-75.
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