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Aplaviroc(AK 602)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aplaviroc(AK 602)图片
规格:98%
分子量:577.71
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
Aplaviroc(AK602),SDP的一个衍生物,是CCR5的拮抗剂,其对HIV-1Ba-L,HIV-1JRFL和HIV-1MOKW的IC50值为0.1-0.4nM。
货号:ajcx12786
CAS:461443-59-4
分子式:C33H43N3O6
分子量:577.71
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Aplaviroc, a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.

Aplaviroc (AK602) is identified as the most potent agent among newly designed and synthesized SDP derivatives. 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. It is of note that Aplaviroc is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. The activity of Aplaviroc's anti-HIV-1 is limited and similar to that seen for zidovudine. Moreover, 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. Aplaviroc 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. Aplaviroc potently blocks rgp120/sCD4 binding to CCR5 with an IC50 value of 2.7 nM. 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].


[1]. Maeda K, et al. Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro. J Virol. 2004 Aug;78(16):8654-62.