DAPTA

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Chemical Structure| 106362-34-9 同义名 : D-Ala-peptide T-amide; Adaptavir; Monomeric (D-Alanine-1) Peptide T amide; mDAPTA; D-Ala-1-peptide T-NH-2; RAP-101; peptide T
CAS号 : 106362-34-9
货号 : A943146
分子式 : C35H56N10O15
纯度 : 98%
分子量 : 856.88
MDL号 : MFCD00076838
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 50 mg/mL(58.35 mM)，配合低频超声助溶
生物活性
靶点

  • CCR

    gp120 Bal-CCR5, IC50:0.06 nM

    CM235-CCR5, IC50:0.32 nM
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... 展开 >>umbia Whitman Walker Clinic Recruiting Washington, District of Columbia, United States, 20009 Principal Investigator: Richard Elion, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.17mL

0.23mL

0.12mL

5.84mL

1.17mL

0.58mL

11.67mL

2.33mL

1.17mL
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