Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist. With IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 17,200 | 10-14周 | ||
50 mg | ¥ 22,800 | 10-14周 | ||
100 mg | ¥ 29,500 | 10-14周 |
产品描述 | Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist. With IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW. |
靶点活性 | CCR5:, HIV-1 (JRFL):0.1 nM, HIV-1 (Ba-L):0.4 nM, HIV-1 (MOKW):0.2 nM |
体外活性 | Aplaviroc (AK602) is identified as the most potent agent among newly designed and synthesized SDP derivatives and it also is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. Aplaviroc exerts potent activity against three wild-type R5 HIV-1 strains (HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW) with IC50 values of 0.1 to 0.4 nM and it potently blocks rgp120/sCD4 binding to CCR5 with an IC50 value of 2.7 nM. The activity of Aplaviroc's anti-HIV-1 is limited and similar to that seen for zidovudine. Aplaviroc suppresses the infectivity and replication of two HIV-1MDR variants, HIV-1MM and HIV-1JSL, at extremely low concentrations (IC50 values of 0.4 to 0.6 nM), while these two R5 HIV-1 variants are less susceptible to zidovudine, nelfinavir, and saquinavir and it also binds to CCR5 with high affinity. The Kd values thus determined for Aplaviroc, E913, E921/TAK-779, and AK671/SCH-C are 2.9±1.0, 111.7±3.5, 32.2±9.6, and 16.0±1.5 nM, respectively. These results suggest that the potent activity of Aplaviroc against R5 HIV-1 stems from its binding to ECL2B and/or its vicinity with high affinity, resulting in inhibition of gp120/CD4 binding to CCR5[1]. |
别名 | AK 602, GW 873140, GSK 873140 |
分子量 | 577.71 |
分子式 | C33H43N3O6 |
CAS No. | 461443-59-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Aplaviroc 461443-59-4 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease CCR AK 602 GW 873140 AK-602 AK602 GW-873140 GSK 873140 GSK-873140 GSK873140 GW873140 Inhibitor inhibitor inhibit