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Cat. No. Product Name CAS No. Information
PC-43512

TAK-779

229005-80-5

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

Discontinued

PC-43448

BMS-707035

729607-74-3

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

PC-43417

Dolutegravir

1051375-16-6

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

Approved

PC-62712

RN-18

431980-38-0

RN-18 is a small molecule that antagonizes HIV-1 Vif function and inhibits HIV-1 replication only in the presence of A3G; increases cellular A3G levels in a Vif-dependent manner and increases A3G incorporation into virions without inhibiting general proteasome-mediated protein degradation; enhances Vif degradation, reduces viral infectivity by increasing A3G incorporation into virions and enhances cytidine deamination of the viral genome.

PC-62244

CX 04328

957890-42-5

CX 04328 (LEDGIN-6) is an allosteric HIV-1 integrase inhibitor that inhibits the LEDGF/p75-integrase interaction with IC50 of 1.37 uM, antiviral activity EC50 of 2.35 uM.

PC-61944

Bictegravir

1611493-60-7

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

PC-61817

MK-8591

865363-93-5

MK-8591 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

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