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CAS No.: 106362-34-9

DAPTA Catalog No. CSN23233

Synonyms: D-Ala-peptide T-amide;Adaptavir;RAP-101

DAPTA is a potent and selective CCR5 antagonist.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The chemokine receptor CCR5 plays a crucial role in transmission of HIV isolates, which predominate in the early and middle stages of infection. DAPTA is a non-toxic experimental antiviral entry inhibitor by selectively targeting CCR5 with potent anti-HIV activities. DAPTA potently inhibited specific CD4-dependent binding of gp120 Bal and CM235 to CCR5 with IC₅₀s of 0.06 nM and 0.32 nM, respectively. DAPTA inhibited the binding of gp120BaL/sCD4 to CCR5 in Cf2Th/synR5 cells with an IC₅₀ of 55 pM. In immunoprecipitation assay, DAPTA (1 nM) blocked the formation of gp120/sCD4 complex with CCR5^[1]. DAPTA increased the Th2 cytokines IL-4, IL-10, and IL-13 and induced a potent virostatic state in infected macrophages in vitro, as well as inhibited production of the proinflammatory cytokines IL-1 and TNFα, which upregulate virus expression^[2].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00951743	HIV Infections	Phase 2	Unknown	July 2010	United States, District of Col... more >>umbia Whitman Walker Clinic Recruiting Washington, District of Columbia, United States, 20009 Principal Investigator: Richard Elion, MD Collapse <<

参考文献

[1] 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
[2] Ruff MR, et al. Update on D-ala-peptide T-amide (DAPTA): a viral entry inhibitor that blocks CCR5 chemokine receptors. Curr HIV Res. 2003 Jan;1(1):51-67

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.1670 mL
- 5.8351 mL
- 11.6703 mL
- 5 mM
- 0.2334 mL
- 1.1670 mL
- 2.3341 mL
- 10 mM
- 0.1167 mL
- 0.5835 mL
- 1.1670 mL

技术信息

CAS号

106362-34-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C35H56N10O15

运输

蓝冰

分子量

856.88

别名

D-Ala-peptide T-amide;Adaptavir;RAP-101;D-Ala-1-peptide T-NH-2;Monomeric (D-Alanine-1) Peptide T amide

溶解度

DMSO	400.0 mg/mL (466.8 mM)
Water	63.0 mg/mL (73.5 mM)

动物实验配方

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