1. GPCR/G Protein
    Immunology/Inflammation
    Anti-infection
  2. CCR
    HIV
  3. DAPTA

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

Cat. No.: HY-P1034 Purity: 95.16%
Handling Instructions

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

For research use only. We do not sell to patients.

Custom Peptide Synthesis

DAPTA Chemical Structure

DAPTA Chemical Structure

CAS No. : 106362-34-9

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1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
25 mg USD 480 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target[2]

gp120BaL/sCD4-CCR5

55 pM (IC50, in Cf2Th/synR5 cells)

gp120CMCM235/sCD4-CCR5

0.32 nM (IC50, in Cf2Th/synR5 cells)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

856.88

Formula

C₃₅H₅₆N₁₀O₁₅

CAS No.
Sequence

Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH2

Sequence Shortening

ASTTTNYT-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1670 mL 5.8351 mL 11.6702 mL
5 mM 0.2334 mL 1.1670 mL 2.3340 mL
10 mM 0.1167 mL 0.5835 mL 1.1670 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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DAPTA
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HY-P1034
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