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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





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




A potent and orally bioavailable HIV-1 protease inhibitor with Ki of 2 nM; exhibits an antiviral EC50 of 30 nM in HIV-1 strain RF-infected CEM-SS cells; also inhibits the proliferation of NSCLC cells, as well as every cell line in the NCI60 cell line panel with mean GI50 of 5.2 uM, induces endoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo.

HIV Infection


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