DAPTA

106362-34-9

C35H56N10O15

H2O : 50 mg/mL (58.35 mM; Need ultrasonic)

Immunology/Inflammation; GPCR/G Protein; Anti-infection

DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities. In Vitro: DAPTA (1 nM) inhibits HIV-1 replication in monocytes/macrophages (M/M) by >90%. DAPTA blocks HIV entry and prevents HIV-1 infection. DAPTA reduces CCR5 mAb binding in human primary macrophages. DAPTA potently blocks R5 gp120-mediated neuronal apoptosis. DAPTA is even more potent in preventing neuronal apoptosis than the CCR5 antagonist TAK-779^[1]. DAPTA potently inhibits specific CD4-dependent binding of gp120 Bal (IC₅₀ = 0.06 nM) and CM235 (IC₅₀ = 0.32 nM) to CCR5. DAPTA (1 nM) blocks formation of the gp120/sCD4 complex with CCR5. DAPTA inhibits the binding of gp120BaL/sCD4 to CCR5 (Cf2Th/synR5) cells with IC₅₀ of 55 +/- 0.08 pM^[2].