Aplaviroc (AK 602), a SDP derivative, is aCCR5antagonist, withIC₅₀sof 0.1-0.4 nM forHIV-1_Ba-L,HIV-1_JRFLandHIV-1_MOKW.

Aplaviroc exerts potent activity against three wild-type R5 HIV-1 strains (HIV-1_Ba-L, HIV-1_JRFLand HIV-1_MOKW) with IC₅₀values 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_MDRvariants, HIV-1_MMand HIV-1_JSL, at extremely low concentrations (IC₅₀values of 0.4 to 0.6 nM). Aplaviroc binds to CCR5 with high affinity. The K_dvalues 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 IC₅₀value 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].

The concentration of Aplaviroc (AK602) reached the maximal concentration immediately after intraperitoneal administration and decreased rapidly^[2].
Aplaviroc (AK602, 60 mg/kg, bid, daily) suppresses R5 HIV-1 viremia in hu-PBMC-NOG mice^[2].

577.71

C₃₃H₄₃N₃O₆

461443-59-4

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Please store the product under the recommended conditions in the Certificate of Analysis.