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TAK-779 is a potent, specific, nonpeptide CCR5 antagonist with Kd of 0.45 nM, antagonizes CCR2b to a lesser extent (27 nM) but does not affect CCR1, CCR3, or CCR4; also blocks the binding of macrophage inflammatory protein 1α and macrophage inflammatory protein 1β to the cells with an IC50 of 1.0 nM; TAK-779 displays highly potent and selective inhibition of the replication of macrophage (M)-tropic HIV-1 (Ba-L strain) in both MAGI-CCR5 cells and PBMCs with EC50 of 1.2 and 3.7 nM, respectively.

HIV Infection





BMS-707035 is a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV IN strand transfer activity with IC50 of 15 nM.

HIV Infection

Phase 2 Discontinued




Dolutegravir (GSK1349572) is a potent, next-generation HIV integrase (IN) inhibitor, inhibits HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM; inhibits HIV-1 replication in PBMCs, MT-4 cells and in the PHIV assay with EC50 of 0.51, 0.71 and 2.2 nM, respectively; demonstrates activity against site-directed molecular clones containing the raltegravir-resistant signature mutations Y143R, Q148K, N155H, and G140S/Q148H; exhibits excellent anti-HIV activity in combination with representative approved antiretroviral agents in vivo.

HIV Infection





Aplaviroc (GSK-873140, GW 873140, AK-602, ONO-4128) is a potent, noncompetitive, allosteric antagonist of the CCR5 receptor with pKb of 8.6; blocks the calcium response effects of CCR5 activation by CCL5, and potently blocks in vitro the infection of R5-tropic HIV-1 (R5-HIV-1) at subnanomolar IC50.

HIV Infection

Phase 3 Discontinued




Bictegravir (GS 9883) is a novel potent HIV-1 integrase (IN) that specifically targets IN strand transfer activity with IC50 of 7.5 nM; exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes with EC50 of 1.5-2.4 nM, with minimal cytotoxicity; exhibits synergistic in vitro antiviral effects in pairwise combinations with tenofovir alafenamide, emtricitabine, or darunavir and maintains potent antiviral activity against HIV-1 variants.

HIV Infection

Phase 3 Clinical




MK-8591 (Islatravir, MK8591, EFdA) is a nucleoside analog that exhibits remarkable potency against wild-type and drug-resistant HIVs, inhibits HIV-1 reverse transcriptase with multiple mechanisms; also retains potent activity against multinucleoside-resistant HIV-2 mutants (EC50<11 nM).

HIV Infection

Phase 2 Clinical




BMS-955176 (GSK-3532795) is a second-generation HIV-1 maturation inhibitor that exhibits potent activity (EC50=3.9±3.4 nM) against a library (n=87) of gag/pr recombinant viruses; exhibits median EC50 of 21 nM toward a library of subtype B clinical isolates assayed in PBMCs; inhibits HIV-1 protease cleavage at the CA/SP1 junction within Gag in VLPs and in HIV-1-infected cells, and binds reversibly and with high affinity to assembled Gag in purified HIV-1 VLPs; has a greatly improved preclinical profile compared to that of Bevirimat.

HIV Infection

Phase 2 Clinical

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