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Antiretroviral prorease Inhibitors

" in MedChemExpress (MCE) Product Catalog:

41

Inhibitors & Agonists

1

Peptides

4

Natural
Products

2

Isotope-Labeled Compounds

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15336
    AG 555

    Tyrphostin AG 555

    		 EGFR Reverse Transcriptase Cancer
    AG 555 (Tyrphostin AG 555), a potent antiretroviral agent, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation .
    AG 555
  • HY-B0249
    Didanosine
    1 Publications Verification

    2',3'-Dideoxyinosine; ddI

    		 HIV Reverse Transcriptase Infection
    Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
    Didanosine
  • HY-15592A
    Cabotegravir sodium
    5 Publications Verification

    GSK-1265744 sodium; S/GSK1265744 sodium

    		 HIV HIV Integrase Infection
    Cabotegravir (GSK-1265744) sodium 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 HIVADA, OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS .
    Cabotegravir sodium
  • HY-153005
    (2RS)-FPMPA

    		HIV Infection
    (2RS)-FPMPA can be used for synthesis of antiretroviral agents against HIV-1 and HIV-2 .
    (2RS)-FPMPA
  • HY-14913
    Apricitabine

    SPD754; AVX754

    		 Nucleoside Antimetabolite/Analog HIV DNA/RNA Synthesis Infection
    Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively . Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection [2].
    Apricitabine
  • HY-P35433
    Tifuvirtide

    T-1249

    		 HIV Inflammation/Immunology
    Tifuvirtide (T-1249) is a peptide human immunodeficiency virus type-1 (HIV-1) fusion inhibitor. Tifuvirtide is a synthetically designed hybrid retroviral envelope polypeptide. Tifuvirtide has antiretroviral activity. Tifuvirtide can be used for the research of HIV infection .
    Tifuvirtide
  • HY-116364
    AZT triphosphate

    3'-Azido-3'-deoxythymidine-5'-triphosphate

    		 HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway .
    AZT triphosphate
  • HY-15592
    Cabotegravir
    5 Publications Verification

    GSK-1265744; S/GSK1265744

    		 HIV HIV Integrase Infection
    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 HIVADA, 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 .
    Cabotegravir
  • HY-116364A
    AZT triphosphate TEA

    3'-Azido-3'-deoxythymidine-5'-triphosphate TEA

    		 HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) TEA is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TEA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TEA also inhibits the DNA polymerase of HBV. AZT triphosphate TEA activates the mitochondria-mediated apoptosis pathway .
    AZT triphosphate TEA
  • HY-116364B
    AZT triphosphate tetraammonium

    3'-Azido-3'-deoxythymidine-5'-triphosphate tetraammonium

    		 HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) tetraammonium is an active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate tetraammonium exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate tetraammonium also inhibits the DNA polymerase of HBV. AZT triphosphate tetraammonium activates the mitochondria-mediated apoptosis pathway .
    AZT triphosphate tetraammonium
  • HY-146017
    HIV-1 inhibitor-22

    		HIV Infection
    HIV-1 inhibitor-22 (compound 11a) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 3.63 μM for HIV-1 RT. HIV-1 inhibitor-22 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 0.304 μM and 0.201 μM, also has low cytotoxicity (CC50 > 227 μM)
    HIV-1 inhibitor-22
  • HY-146015
    HIV-1 inhibitor-21

    		HIV Infection
    HIV-1 inhibitor-21 (compound 9b) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 0.55 μM for HIV-1 RT. HIV-1 inhibitor-21 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 12.7 nM and 10.4 nM, and has relatively low cytotoxicity (MT-4 cells CC50 =10.2 μM) .
    HIV-1 inhibitor-21
  • HY-14920
    Dexelvucitabine

    Reverset; d-d4FC

    		 Reverse Transcriptase HIV Infection
    Dexelvucitabine (Reverset; d-d4FC), a Cytidine (HY-B0158) analog, is an orally active nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful agent against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-Deoxycytidine antiretroviral agent .
    Dexelvucitabine
  • HY-17003
    Saquinavir mesylate
    Maximum Cited Publications
    10 Publications Verification

    Ro 31-8959/003

    		 HIV HIV Protease Autophagy Infection Cancer
    Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy.
    Saquinavir mesylate
  • HY-146365
    HIV-1 inhibitor-30

    		HIV Infection Inflammation/Immunology
    HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS .
    HIV-1 inhibitor-30
  • HY-W013441
    2',3'-Dideoxyadenosine

    		HIV Infection
    2',3'-Dideoxyadenosine is an inhibitor of HIV replication . Antiretroviral activity . Antiviral efficacy .
    2',3'-Dideoxyadenosine
  • HY-N8379
    Morolic acid

    		Others Others
    Morolic acid (compound 6) can be isolated from Phoradendron brachystachyum DC Nutt. Morolic acid has antiretroviral activity .
    Morolic acid
  • HY-17431
    Fosamprenavir Calcium Salt
    4 Publications Verification

    GW433908G

    		 HIV Endogenous Metabolite Infection
    Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility . Anti-HIV infection .
    Fosamprenavir Calcium Salt
  • HY-78726
    Fosamprenavir
    4 Publications Verification

    Amprenavir phosphate; GW 433908

    		 HIV Endogenous Metabolite Infection
    Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility . Anti-HIV infection .
    Fosamprenavir
  • HY-155095
    DNA polymerase-IN-4

    		Others Infection
    DNA polymerase-IN-4 (Compd 5c), a coumarin derivative, has antiretroviral activity with IC50 value of 134.22 μM .
    DNA polymerase-IN-4
  • HY-17007
    Saquinavir
    Maximum Cited Publications
    10 Publications Verification

    Ro 31-8959

    		 HIV HIV Protease SARS-CoV Infection Cancer
    Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.36 μM.
    Saquinavir
  • HY-131596
    Emtricitabine triphosphate

    (-)-Emtricitabine triphosphate

    		 HIV Infection
    Emtricitabine triphosphate ((-)-Emtricitabine triphosphate) is the phosphorylated anabolite of Emtricitabine (HY-17427). Emtricitabine is a nucleoside reverse transcriptase inhibitor. Emtricitabine is antiretroviral agent for HIV and HBV infection .
    Emtricitabine triphosphate
  • HY-78726S
    Fosamprenavir-d4

    Amprenavir phosphate-d4; GW 433908-d4

    		 Isotope-Labeled Compounds HIV Endogenous Metabolite Infection
    Fosamprenavir-d4 is deuterium labeled Fosamprenavir. Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility[1]. Anti-HIV infection[1].
    Fosamprenavir-d4
  • HY-136548B
    Tenofovir diphosphate disodium
    1 Publications Verification

    TFV-DP disodium

    		 HIV Infection Inflammation/Immunology
    Tenofovir diphosphate disodium is an antiretroviral agent and an inhibitor of DNA polymerases. Tenofovir diphosphate disodium is a substrate of HIV-1 reverse transcriptase (RT). Tenofovir diphosphate disodium can be used for the research of Aids .
    Tenofovir diphosphate disodium
  • HY-100079
    9-Propenyladenine

    Mutagenic Impurity of Tenofovir Disoproxil; Tenofovir Impurity 2

    		 HIV Infection
    9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral agent known as nucleotide analogue reverse transcriptase inhibitors, which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
    9-Propenyladenine
  • HY-17431R
    Fosamprenavir Calcium Salt (Standard)

    GW433908G (Standard)

    		 HIV Endogenous Metabolite Infection
    Fosamprenavir (Calcium Salt) (Standard) is the analytical standard of Fosamprenavir (Calcium Salt). This product is intended for research and analytical applications. Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility . Anti-HIV infection .
    Fosamprenavir Calcium Salt (Standard)
  • HY-100079A
    (Z)-9-Propenyladenine

    (Z)-Mutagenic Impurity of Tenofovir Disoproxil

    		 HIV Infection
    (Z)-9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral agent known as nucleotide analogue reverse transcriptase (NtART) inhibitor, which blocks reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
    (Z)-9-Propenyladenine
  • HY-17007S
    Saquinavir-d9

    		Isotope-Labeled Compounds HIV HIV Protease SARS-CoV Infection Cancer
    Saquinavir-d9 is the deuterium labeled Saquinavir. Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.36 μM[1][2].
    Saquinavir-d9
  • HY-111964
    Lenacapavir
    5 Publications Verification

    GS-6207

    		 HIV Infection
    Lenacapavir (GS-6207) is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs) . Lenacapavir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Lenacapavir
  • HY-14267
    Lersivirine

    UK-453061

    		 HIV Reverse Transcriptase Infection
    Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC50=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains .
    Lersivirine
  • HY-100079R
    9-Propenyladenine (Standard)

    Mutagenic Impurity of Tenofovir Disoproxil (Standard); Tenofovir Impurity 2 (Standard)

    		 HIV Infection
    9-Propenyladenine (Standard) is the analytical standard of 9-Propenyladenine. This product is intended for research and analytical applications. 9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral agent known as nucleotide analogue reverse transcriptase inhibitors, which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
    9-Propenyladenine (Standard)
  • HY-B0116
    Stavudine
    3 Publications Verification

    d4T

    		 Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis .
    Stavudine
  • HY-B0116A
    Stavudine sodium

    d4T sodium

    		 Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis .
    Stavudine sodium
  • HY-125028
    Hck-IN-1

    		Src HIV Infection
    Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity .
    Hck-IN-1
  • HY-125810
    4'-Ethynyl-2'-deoxyadenosine

    		HIV Reverse Transcriptase Infection Inflammation/Immunology
    4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    4'-Ethynyl-2'-deoxyadenosine
  • HY-122470
    Stampidine

    		Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively .
    Stampidine
  • HY-153094
    BDM-2

    		HIV HIV Integrase 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 .
    BDM-2
  • HY-146019
    HIV-1 inhibitor-24

    		HIV Infection
    HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety .
    HIV-1 inhibitor-24
  • HY-121075
    Alizarin complexone

    		Reverse Transcriptase Infection
    Alizarin complexone is a calcium-tracer and a chelating agent. Alizarin complexone is Rous-associated virus 2 reverse transcriptase (RAV-2 RT) inhibitor .
    Alizarin complexone
  • HY-109014
    Tenofovir exalidex

    CMX-157

    		 HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
    Tenofovir exalidex
  • HY-146019A
    HIV-1 inhibitor-25

    		HIV Infection
    HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
    HIV-1 inhibitor-25

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