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Aplaviroc hydrochloride

CAS No. : 461023-63-2

MCE 站：Aplaviroc hydrochloride

产品活性：Aplaviroc (AK 602) hydrochloride，SDP的一个衍生物，是 CCR5 的拮抗剂，其对 HIV-1_Ba-L， HIV-1_JRFL 和 HIV-1_MOKW 的 IC₅₀ 值为 0.1-0.4 nM。

研究领域：GPCR/G Protein  |  Immunology/Inflammation  |  Anti-infection

作用靶点：CCR  |  HIV

In Vitro: Aplaviroc exerts potent activity against three wild-type R5 HIV-1 strains (HIV-1_Ba-L, HIV-1_JRFL and HIV-1_MOKW) with IC₅₀ values of 0.1 to 0.4 nM. Aplaviroc is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. Aplaviroc suppresses the infectivity and replication of two HIV-1_MDR variants, HIV-1_MM and HIV-1_JSL, at extremely low concentrations (IC₅₀ values of 0.4 to 0.6 nM). Aplaviroc binds to CCR5 with high affinity. The K_d 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.

In Vivo: The concentration of Aplaviroc (AK602) reached the maximal concentration immediately after intraperitoneal administration and decreased rapidly.
Aplaviroc (AK602, 60 mg/kg, bid, daily) suppresses R5 HIV-1 viremia in hu-PBMC-NOG mice.

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