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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-DAPTA
DAPTA

Chemical Structure : DAPTA

CAS No.: 106362-34-9

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DAPTA (D-ala-peptide T-amide, Adaptavir)

货号: PC-21104Not For Human Use, Lab Use Only.

DAPTA (D-ala-peptide T-amide, Adaptavir) is an HIV gp120-derived CCR5 entry inhibitor, inhibits CCR5-mediated monocyte migration and attenuates neuroinflammation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

DAPTA (D-ala-peptide T-amide, Adaptavir) is an HIV gp120-derived CCR5 entry inhibitor, inhibits CCR5-mediated monocyte migration and attenuates neuroinflammation, shows potent anti-HIV activities.
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 pM.
DAPTA administration significantly decreased marble burying and repetitive behavior in BTBR mice.
DAPTA treatment inhibited CCR5+, CD4+CCR5+, CCR5+IL-6+, CCR5+IL-9+, CCR5+IL-17A+, CCR5+RORγT+, and upregulated CCR5+IL-10+, and CCR5+Foxp3+ production.
DAPTA downregulated IL-6, IL-9, IL-17A, and RORγT, and increased IL-10 and Foxp3 protein and mRNA expression.

物理化学性质&存储条件

分子量 856.89
分子式 C35H56N10O15
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-2-((2S,5S,8S,11S,14R)-14-amino-2,5,8-tris((R)-1-hydroxyethyl)-11-(hydroxymethyl)-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecanamido)-N1-((S)-1-(((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)succinamide

参考文献

1. Ahmad SF, et al. Eur J Pharmacol. 2019 Mar 5;846:100-108.

2. Pollicita M, et al. Antivir Chem Chemother. 2007;18(5):285-95.

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