Search Result
Results for "
HIV-1 integrase
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107485
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-
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- HY-13025
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HIV
HIV Integrase
|
Infection
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HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-150079
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HIV Integrase
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Infection
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HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1) .
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- HY-159092
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HIV Integrase
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Infection
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HIV-1 integrase inhibitor 13 (Compound 15) is an inhibitor for HIV-1 integrase with an IC50 of 1.8 nM. HIV-1 integrase inhibitor 13 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 21 and 580 nM, respectively .
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- HY-130760
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HIV Integrase
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Infection
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HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC50 of 33.3 nM .
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- HY-108817
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HIV Integrase
HIV
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Infection
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HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.
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-
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- HY-108820
-
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HIV Integrase
HIV
|
Infection
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HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
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-
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- HY-W507252
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HIV Integrase
|
Infection
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HIV-1 integrase inhibitor 11 (compound 5) is a potent inhibitor of HIV-1 integrase, with the IC50 of 125 μM .
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- HY-159091
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HIV Integrase
|
Infection
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HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
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- HY-132572
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HIV
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Infection
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HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC50 of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity .
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- HY-N7330
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HIV Integrase
HIV
|
Infection
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Integracin B is a potent dimeric alkyl aromatic inhibitor of HIV-1 integrase discovered from the screening of fungal extracts using an in vitro assay. Integracin B inhibits both coupled and strand transfer activity of HIV-1 integrase .
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- HY-W103287
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HIV Integrase
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Infection
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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 .
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- HY-16907
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S/GSK-364735
|
HIV
HIV Integrase
|
Infection
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GSK-364735 is a potent antiretroviral agent against human immunodeficiency virus type 1 (HIV-1) and serves as an integrase inhibitor with an IC50 of 8 ± 2 nM. GSK-364735 can be utilized in antiviral research .
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- HY-12108
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|
HIV Integrase
HIV
|
Infection
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S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase (
IC50: 20 nM). The EC50, and CC50 of S 1360
in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants .
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- HY-108935
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HIV Integrase
GLUT
Tyrosinase
|
Cancer
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Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases .
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- HY-12210
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HIV Integrase
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Infection
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(S)-BI-1001 (Compound 11) is an active S-enantiomer of BI-1001. (S)-BI-1001 exhibits antiviral potency against HIV-1 integrase with an IC50 of 28 nM, an EC50 of 450 nM and a Kd of 4.7 μM .
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- HY-130000
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STP0404
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HIV Integrase
HIV
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Infection
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Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties .
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- HY-13269
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|
HIV
HIV Integrase
|
Infection
Inflammation/Immunology
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BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1) .
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- HY-134851
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HIV
|
Infection
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HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
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- HY-18595
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|
HIV
HIV Integrase
|
Infection
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BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.
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- HY-17605
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- HY-147653
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HIV Integrase
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Infection
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Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432 .
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- HY-N0457A
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(-)-Chicoric acid; trans-Caffeoyltartaric acid
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HIV Integrase
HIV
Endogenous Metabolite
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Infection
Cancer
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L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
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- HY-163177
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HIV
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Infection
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HIV-1 inhibitor-63 (compound S17) is a potent HIV-1 inhibitor. HIV-1 inhibitor-63 inhibits integrase-Ku70 complex formation with an IC50 value of 12 µM. HIV-1 inhibitor-63 inhibits HIV-1 post-integration DNA repair .
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- HY-17605A
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GS-9883 sodium
|
HIV Integrase
HIV
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Infection
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Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
|
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- HY-B1408
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2-Hydroxybenzanilide
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HIV Integrase
HIV
|
Infection
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Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus
by targeting HIV-1 integrase or reverse transcriptase.
|
-
-
- HY-N11288
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|
HIV
|
Infection
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Methyl salvionolate A is a potent inhibitor of HIV-1. Methyl salvionolate A inhibits P24 antigen in HIV-1 infected MT-4 cell with an EC50 of 1.62 μg/ml. Methyl salvionolate A also inhibits HIV-1 reverse transcriptase, protease and integrase with
IC50s of 50.58, 10.73 and 7.58 μg/ml, respectively .
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- HY-N0457AR
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HIV Integrase
HIV
Endogenous Metabolite
|
Infection
Cancer
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L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
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- HY-13238
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Dolutegravir
Maximum Cited Publications
23 Publications Verification
S/GSK1349572
|
HIV Integrase
HIV
|
Infection
|
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) .
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- HY-17605R
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HIV
HIV Integrase
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Infection
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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.
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- HY-17605S1
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- HY-17605S2
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GS-9883-d4
|
HIV
HIV Integrase
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Infection
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Bictegravir-d4 is a deuterium of Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
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- HY-13238A
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S/GSK1349572 sodium
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HIV Integrase
HIV
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Infection
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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) .
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- HY-13238R
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HIV Integrase
HIV
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Infection
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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) .
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- HY-13238S1
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S/GSK1349572-d3
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Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
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Dolutegravir-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)[1][2].
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- HY-13238S2
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S/GSK1349572-d5
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Isotope-Labeled Compounds
HIV Integrase
HIV
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Infection
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Dolutegravir-d5 is 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)[1][2].
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- HY-100083
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HIV
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Others
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Dolutegravir intermediate-1 is a synthetic intermediate of Dolutegravir extracted from patent WO 2016125192 A2. Dolutegravir is an integrase inhibitor developed for the treatment of human immunodeficiency virus (HIV)-1 infection.
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- HY-122229
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HIV
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Infection
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GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
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- HY-161945
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HIV
HIV Integrase
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Infection
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IN-RNA-IN-2 (compound 1a) is an inhibitor (IC50=70 nM) of the interaction between HIV-1 integrase and the viral RNA genome. IN-RNA-IN-2 exerts its anti-HIV activity by inhibiting the viral replication process .
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- HY-153094
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HIV
HIV Integrase
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Infection
|
BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity .
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- HY-17605S
-
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Isotope-Labeled Compounds
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Infection
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Bictegravir- 15N,d2 (GS-9883- 15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605) . Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
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- HY-153247
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- HY-150080
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BMS-986180
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HIV
HIV Integrase
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Infection
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GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
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- HY-N6711
-
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HIV Integrase
Bacterial
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Infection
Metabolic Disease
|
Equisetin is an N-methylserine-derived acyltramic acid isolated from the terrestrial fungus Fusarium equiseti NRRL 5537. As a tetrad-containing natural product, it has antibacterial and antiviral activities, inhibiting the growth of Gram-positive bacteria and HIV-1 integrase activity, but not Gram-negative bacteria. Equisetin is a quorum sensing inhibitor (QSI) that attenuates the QS-regulated virulence phenotype in Pseudomonas aeruginosa without affecting bacterial growth, and is a leading compound for studying Pseudomonas aeruginosa infection. In addition, equisetin inhibits the enzymatic activity of 11b-hydroxysteroid dehydrogenase type 1 (11b-HSD1) without affecting food intake, blood pressure, or heart rate, exerting anti-obesity effects on adipose tissue .
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- HY-18666
-
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HIV
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Infection
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D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
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- HY-14740
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GS-9137; JTK-303; D06677
|
HIV Integrase
HIV
|
Infection
|
Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
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- HY-14740S
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GS-9137-d8; JTK-303-d8; D06677-d8
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
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-
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- HY-14740R
-
|
HIV Integrase
HIV
|
Infection
|
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-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13238S1
-
|
Dolutegravir-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)[1][2].
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-
-
- HY-17605S
-
|
Bictegravir- 15N,d2 (GS-9883- 15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605) . Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
|
-
-
- HY-17605S1
-
|
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-17605S2
-
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Bictegravir-d4 is a deuterium of Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
|
-
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- HY-13238S2
-
|
Dolutegravir-d5 is 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)[1][2].
|
-
-
- HY-14740S
-
|
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
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Cat. No. |
Product Name |
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Classification |
-
- HY-13025
-
|
|
Azide
|
HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
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