DAPTA(Synonyms: D-Ala-peptide T-amide Adaptavir) | Cytiva思拓凡-Whatman滤纸滤膜滤器

DAPTA;(Synonyms: D-Ala-peptide T-amide; Adaptavir) 纯度: 95.16%

DAPTA 是一种合成肽，为 CCR5 抑制剂，同时具有抗 HIV 的活性。

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

DAPTA Chemical Structure

CAS No. : 106362-34-9

规格	价格	是否有货	数量
1 mg	￥700	In-stock
5 mg	￥1300	In-stock
10 mg	￥2200	In-stock
25 mg	￥4100	In-stock
50 mg	;	询价	;
100 mg	;	询价	;

* Please select Quantity before adding items.

DAPTA 相关产品

bull;相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Peptide Library

生物活性

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

IC₅₀ Target^[2]

gp120_BaL/sCD4-CCR5

55 pM (IC₅₀, in Cf2Th/synR5 cells)

gp120CM_CM235/sCD4-CCR5

0.32 nM (IC₅₀, in Cf2Th/synR5 cells)

体外研究
(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.

分子量

856.88

Formula

C₃₅H₅₆N₁₀O₁₅

CAS 号

106362-34-9

Sequence

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

Sequence Shortening

ASTTTNYT-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-80deg;C	2 years
	-20deg;C	1 year
In solvent	-80deg;C	6 months
	-20deg;C	1 month

溶解性数据

In Vitro:;

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

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

[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.

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.
参考文献	[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.

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.

参考文献

[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.