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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]. |
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 << |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 106362-34-9 |
分子式 | C35H56N10O15 |
分子量 | 856.877 |
别名 | 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 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
H2O: 50 mg/mL(58.35 mM),配合低频超声助溶 |
动物实验配方 |