Adaptavir (DAPTA)

製品コードS8501 バッチS850101

印刷

化学情報

Chemical Structure Synonyms D-Ala-peptide T-amide, peptide T Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C35H56N10O15
分子量 856.88 CAS No. 106362-34-9
Solubility (25°C)* 体外 Water 100 mg/mL (116.7 mM)
 
 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
in vitro 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[1]. 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[2].
in vivo The levels of inflammatory cytokines IL-1, IL-6, and TNFα decrease in plasma following DAPTA treatment[2]. Peptide T(DAPTA) treatment prevents the neuronal cell death associated with gpl20. DAPTA prevents gpl20-associated neural deficits in vivo[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Monocyte-derived macrophages
濃度 10−12 to 10−7 M
反応時間 7 days and 14 days
実験の流れ

MDM (Monocyte-derived macrophages) at a concentration of 1×106 cells per ml in 24-well plates are cultured for 7-14 days in growth medium (RPMI, 5% human AB serum). At the beginning of the experiment the cells are washed with serum free RPMI and are treated with peptide T (DAPTA) at the indicated concentrations, or vehicle (medium), for 1-2 h at 37 °C, 5% CO2. Cultures are washed two times to remove unabsorbed virus and cultured in growth medium containing peptide T at indicated concentrations. Supernatants from day 7 or 14 cultured MDM's are sampled. Cultures are re-fed with peptide T and 50% fresh medium after the day 7 sample. The p24 antigen determination is made using commercial kits.
動物実験 動物モデル Sprague-Dawley rats
投薬量 5 μg/100 μl
投与方法 s.c.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cancer associated fibroblast-derived CCL5 promotes hepatocellular carcinoma metastasis through activating HIF1α/ZEB1 axis [ Cell Death Dis, 2022, 13(5):478] PubMed: 35589690
Chemokine CCL5 promotes robust optic nerve regeneration and mediates many of the effects of CNTF gene therapy [ Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118] PubMed: 33627402
Cholesterol impacts chemokine CCR5 receptor ligand-binding activity [ FEBS J, 2020, 287(11):2367-2385] PubMed: 31738467

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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