HIV Integrase

Related Products

HIV integrase is one of the three key enzymes of the pol gene of HIV. HIV integrase catalyzes the insertion into the genome of the infected human cell of viral DNA produced by the retrotranscription process. This unique step in the virus life cycle provides a variety of points for intervention and hence is an attractive target for the development of new therapeutics for the treatment of AIDS. HIV integrase includes HIV-1 and HIV-2 integrases.

HIV-1 integrase is a 32-kDa enzyme that carries out DNA integration in a two-step reaction. In the first step, called 3′ processing, two nucleotides are removed from each 3′ end of the viral DNA made by reverse transcription. In the next step, called DNA strand transfer, a pair of transesterification reactions integrates the ends of the viral DNA into the host genome. Integrase is comprised of three structurally and functionally distinct domains, and all three domains are required for each step of the integration reaction.

HIV Integrase Inhibitors (72)

HIV Integrase Related Products (73):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-17605S1

Bictegravir-d₅	Inhibitor
Bictegravir-d₅ is deuterated labeled Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC₅₀ of 7.5 nM.

HY-15592R

Cabotegravir (Standard)	Inhibitor
Cabotegravir (Standard) is the analytical standard of Cabotegravir. This product is intended for research and analytical applications. Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer 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 HIV_ADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS.

HY-14740S1

Elvitegravir-d₆	Inhibitor
Elvitegravir-d₆ (GS-9137-d₆) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) 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, respectively.

HY-W103287

2-Hydroxyisoquinoline-1,3(2H,4H)-dione	Inhibitor
Hydroxyisoquinoline-1,3(2H,4H)-dione (compound 6a) is a HIV-1 integrase (IN) and HIV-1 reverse transcriptase (RT) ribonuclease H (RNase H) inhibitor with an IC₅₀ value of 6.32, 5.9 µM, respectively.

HY-10353AS2

Raltegravir-d₄ potassium	Inhibitor
Raltegravir-d₄ (potassium) (MK 0518-d₄ (potassium)) is deuterium labeled Raltegravir (potassium). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.

HY-14740R

Elvitegravir (Standard)	Inhibitor
Elvitegravir (Standard) is the analytical standard of Elvitegravir. This product is intended for research and analytical applications. Elvitegravir (GS-9137; JTK-303; D06677) 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, respectively.

HY-10353AR

Raltegravir (potassium) (Standard)	Inhibitor
Raltegravir (potassium) (Standard) is the analytical standard of Raltegravir (potassium). This product is intended for research and analytical applications. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.

HY-17605S4

Bictegravir-d₇	Inhibitor
Bictegravir-d₇ (GS-9883-d₇) is deuterium labeled Bictegravir. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC₅₀ of 7.5 nM.

HY-14740S2

Elvitegravir-¹³C₆	Inhibitor
Elvitegravir-¹³C₆ (GS-9137-¹³C₆) is ¹³C labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) 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, respectively.

HY-16907B

GSK-364735 sodium	Inhibitor
GSK-364735 sodium (S/GSK-364735 sodium) is the sodium salt form of GSK-364735 (HY-16907). GSK-364735 sodium is an antiretroviral, that inhibits the integrase of human immunodeficiency virus type 1 (HIV-1) with an IC₅₀ of 7.8 nM.

HY-13238R

Dolutegravir (Standard)	Inhibitor
Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. 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).

HY-17605R

Bictegravir (Standard)	Inhibitor
Bictegravir (Standard) is the analytical standard of Bictegravir. This product is intended for research and analytical applications. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC₅₀ of 7.5 nM.

HY-W749636

N-De-2,4-difluorobenzyl dolutegravir	Inhibitor
N-De-2,4-difluorobenzyl dolutegravir is a metabolite of Dolutegravir (HY-13238). Dolutegravir is a HIV integrase inhibitor inhibitor.

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