HIV Integrase

CAS No.	Product Name	Inquiry
	Dolutegravir-d3 Dolutegravir-d3 (S/GSK1349572-d3) is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50 =3.6-5.8 nM).
	Dolutegravir-d6-sodium Dolutegravir-d6 sodium (S/GSK1349572-d6 sodium) is the deuterium labeled Dolutegravir sodium. Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
	Elvitegravir-d8 Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB , HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
	HIV-1-protease-IN-6 HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild. type virus
	HIV-1-protease-IN-7 HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor (IC50=3.52 nM, EC50=37 nM).
	HIV-Protease-Substrate-1-TFA HIV Protease Substrate 1 TFA, a fiuorogenic HIV protease substrate, can be used to study enzymatic activity of HIV protease.
1000287-05-7	TMC310911 TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity.
1051375-13-3	Cabotegravir-sodium Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively.
1155419-89-8	BI 224436 BI 224436 is a novel HIV-1 non-catalytic-site integrase inhibitor; has antiviral EC50s of <15 nM against different HIV-1 laboratory strains and cellular cytotoxicity of >90 μM.
1246816-98-7	Raltegravir-[d3] Potassium Salt Labelled Raltegravir K salt. Raltegravir is a potent, selective, and orally bioavailable inhibitor of HIV integrase (IC50 = 15 nM). It is metabolized primarily by uridine diphosphate glucuronosyltransferase 1A. Raltegravir has long-term efficacy and safety in managing HIV-1 infection in adults, children, and adolescents.
1051375-19-9	Dolutegravir sodium Dolutegravir sodium salt is a HIV integrase inhibitor(IC50= 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
871038-72-1	Raltegravir Potassium Salt Raltegravir is a potent, selective, and orally bioavailable inhibitor of HIV integrase (IC50 = 15 nM). It is metabolized primarily by uridine diphosphate glucuronosyltransferase 1A. Raltegravir has long-term efficacy and safety in managing HIV-1 infection in adults, children, and adolescents.
1051375-16-6	Dolutegravir Dolutegravir is a two-metal-binding HIV-1 integrase inhibitor with IC50 of 2.7 nM, with modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. It blocks the strand transfer step of the integration of the viral genome into the host cell (INSTI).
697761-98-1	Elvitegravir Elvitegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
1051375-10-0	Cabotegravir (GSK744, GSK1265744) Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.
1807988-02-8	Bictegravir sodium Bictegravir sodium is a HIV-1 integrase strand transfer inhibitor that is derived from the drug dolutegravir.
518048-05-0	Raltegravir Raltegravir is a potent integrase (IN) inhibitor used as an antiretroviral medication for the treatment of HIV infections.
224186-05-4	Integracin B It is an unusual ester of two structurally related alkylresorcinols first isolated from fungus, cytonaema sp. It is a potent inhibitor of HIV-1.
1611493-60-7	Bictegravir Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM for strand transfer activity. Bictegravir is a drug of the integrase inhibitor class that was copied from Dolutegravir by scientists at Gilead Sciences. Bictegravir also inhibits HIV-1 viral infection in MT-2 and MT-4 cells, CD4+ T cells, and macrophages (EC50s = 1.5, 2.5, 1.5, and 6.6 nM, respectively) without exhibiting cytotoxicity (CC50s = 10.3, 3.7, 13, and 29.8 μM, respectively). In 2016, bictegravir was in a Phase 3 trial as part of a single tablet regimen in combination with tenofovir alafenamide (TAF) and emtricitabine (FTC) for the treatment of HIV-1 infection.

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