Adaptavir (DAPTA)

製品コードS8501 バッチS850101

化学情報

	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	Adaptavir (DAPTA) is a non-toxic experimental antiviral entry inhibitor. It 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^[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	Adaptavir (DAPTA) treatment decreases the levels of inflammatory cytokines IL-1, IL-6, and TNFα in plasma^[2]. It prevents the neuronal cell death associated with gpl20 and 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 Adaptavir (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 this compound at indicated concentrations. Supernatants from day 7 or 14 cultured MDM's are sampled. Cultures are re-fed with it 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.

参考

https://pubmed.ncbi.nlm.nih.gov/16002156/
https://pubmed.ncbi.nlm.nih.gov/15043212/
https://pubmed.ncbi.nlm.nih.gov/8461978/

https://pubmed.ncbi.nlm.nih.gov/11530189/

+ 展开

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。