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DAPTA (Synonyms: D-Ala-peptide T-amide; Adaptavir)

Katalog-Nr.GC17040

DAPTA ist ein synthetisches Peptid, wirkt als Viruseintrittshemmer, indem es selektiv auf CCR5 abzielt, und zeigt starke Anti-HIV-AktivitÄten.

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DAPTA Chemische Struktur

Cas No.: 106362-34-9

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1mg
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5mg
99,00 $
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10mg
171,00 $
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25mg
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Sample solution is provided at 25 µL, 10mM.

Description of DAPTA

DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.

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].

References:
[1]. Pollicita M, et al. Profound anti-HIV-1 activity of DAPTA in monocytes/macrophages and inhibition of CCR5-mediated apoptosis in neuronal cells. Antivir Chem Chemother. 2007;18(5):285-95.
[2]. Polianova MT, et al. Chemokine receptor-5 (CCR5) is a receptor for the HIV entry inhibitor peptide T (DAPTA). Antiviral Res. 2005 Aug;67(2):83-92.

Protocol of DAPTA

Kinase experiment:

A novel FITC-labeled tracer from soluble gp120 proteins (25 g/mL) is prepared using a Fluorescent protein labeling kit, according to the manufacture's instructions. Uncoupled FLUOS is removed by Sephadex G-10 column filtration. The molar ratio between FLUOS-labeling molecules and protein is from 3.5 to 4.5 fluorescence molecules per molecule of gp120. The concentration of fluorescent-labeled proteins is measured by Bradford assay and Western blotting by using calibrating amounts of soluble molecules with known concentration. Binding assays are performed in binding buffer, in final volume 100l. Binding is carried out for 1 h at 37°C in 96-well filter plates. Unbound-labeled proteins are removed by rapid vacuum filtration and ishing using a 96-well plates manifold. Each binding mix is washed five times with 0.2 mL (total volume of 1.0 mL/well) cold ishing buffer (50 mM HEPES, pH 7.4, 150 mM NaCl, 5 mM MgCl2, 1 mM CaCl2). Filters are counted with a fluorescent plate reader at 495/530 nm.

References:

[1]. Pollicita M, et al. Profound anti-HIV-1 activity of DAPTA in monocytes/macrophages and inhibition of CCR5-mediated apoptosis in neuronal cells. Antivir Chem Chemother. 2007;18(5):285-95.
[2]. Polianova MT, et al. Chemokine receptor-5 (CCR5) is a receptor for the HIV entry inhibitor peptide T (DAPTA). Antiviral Res. 2005 Aug;67(2):83-92.

Chemical Properties of DAPTA

Cas No. 106362-34-9 SDF
Überlieferungen D-Ala-peptide T-amide; Adaptavir
Formula C35H56N10O15 M.Wt 856.89
Löslichkeit Soluble to 1 mg/ml in sterile water Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of DAPTA

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.167 mL 5.8351 mL 11.6701 mL
5 mM 0.2334 mL 1.167 mL 2.334 mL
10 mM 0.1167 mL 0.5835 mL 1.167 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 14 reference(s) in Google Scholar.)

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