Search Result
Results for "
nonnucleoside reverse transcriptase
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-19509
-
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Reverse Transcriptase
HIV
|
Infection
|
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IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM .
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-
-
- HY-15379
-
|
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HIV
|
Infection
|
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Atevirdine is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Atevirdine inhibits non-nucleoside reverse transcriptase that leads to viral multiplication .
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-
-
- HY-90005
-
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R165335; TMC125
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Reverse Transcriptase
HIV
|
Infection
|
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Etravirine (R165335; TMC125) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
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-
-
- HY-118423
-
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IQP-0410
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HIV
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Inflammation/Immunology
|
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SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase . SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism .
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-
-
- HY-19925
-
|
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HIV
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Infection
|
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AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
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-
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- HY-148248
-
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HIV
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Infection
|
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BI-2540 is a HIV non-nucleoside reverse transcriptase (NNRT) inhibitor .
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-
-
- HY-118632
-
|
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Reverse Transcriptase
HIV
|
Infection
|
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BILR 355 is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). BILR 355 is highly specific toward HIV-1 reverse transcriptase (RT). BILR 355 can be used for HIV infections research .
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-
-
- HY-169207
-
-
-
- HY-107001
-
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(S)-DPC 961; DMP 961
|
HIV
Reverse Transcriptase
|
Infection
|
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DPC 961 (DMP 961) is a non-nucleoside reverse transcriptase inhibitor (NNRTI). DPC 961 is a potent and specific inhibitor of HIV-1 reverse transcriptase, which inhibits the activity of HIV-1 reverse transcriptase in a non-competitive manner, thereby preventing viral replication. DPC 961 can be used for research on AIDS .
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-
-
- HY-139158
-
|
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HIV
|
Infection
|
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Ainuovirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). Ainuovirine inhibits HIV replication by non-competitively binding to HIV reverse transcriptase and blocking the reverse transcription process of viral RNA. Ainuovirine can be used for human immunodeficiency virus (HIV) type 1 infection .
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-
-
- HY-130241
-
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HIV
|
Infection
|
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Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme .
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-
-
- HY-10570
-
-
-
- HY-90005S
-
|
TMC-125 d4; R-165335 d4
|
Reverse Transcriptase
HIV
|
Infection
|
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Etravirine-d4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
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-
-
- HY-142073
-
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DHCal A; NSC 678323
|
Reverse Transcriptase
HIV
|
Infection
|
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(+)-Dihydrocalanolide A (DHCal A; NSC 678323) is an orally active nonnucleoside inhibitor of Reverse Transcriptase. (+)-Dihydrocalanolide A can be used to HIV infection research .
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-
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- HY-125433
-
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HIV
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Infection
|
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A-75925 is a human immunodeficiency virus type 1 (HIV-1) proteinase inhibitor and can be utilized in HIV-1 rersearch .
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-
-
- HY-14266
-
|
TMC120; R147681
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
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Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations .
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-
-
- HY-16767
-
Doravirine
Maximum Cited Publications
10 Publications Verification
MK-1439
|
HIV
Reverse Transcriptase
|
Infection
|
|
Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
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-
-
- HY-15355
-
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R 89439
|
Reverse Transcriptase
HIV
|
Infection
|
|
Loviride (R 89439) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), with an IC50 of 0.3 μM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells .
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-
-
- HY-149338
-
|
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HIV Protease
|
Infection
|
|
NNRT-IN-3 (compound 8) is an HIV-1 non-nucleoside reverse transcriptase inhibitor (EC50=0.01 μM) .
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-
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- HY-117477
-
|
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Reverse Transcriptase
HIV
|
Infection
|
|
DPC-963 is an oral active non-nucleoside reverse transcriptase inhibitor with the IC50 of 18 nM. DPC-963 can be used for study of HIV .
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-
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- HY-129667
-
|
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Reverse Transcriptase
HIV
|
Infection
|
|
BM 21.1298 is a selective and high specific nonnucleoside immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) inhibitor with antiviral activity .
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-
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- HY-14294
-
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S-1153
|
Reverse Transcriptase
HIV
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Infection
|
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Capravirine (S-1153) is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent antiviral activity. Capravirine inhibits replication of HIV-1 strains that are resistant to nucleoside/nucleotide reverse transcriptase inhibitors and other NNRTIs. Capravirine is metabolized by the cytochrome P450 enzyme CYP3A4 .
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-
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- HY-132508S
-
-
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- HY-146031
-
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HIV
|
Infection
|
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A3N19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with an EC50 of 3.28 nM against HIV-1 IIIB .
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-
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- HY-147411
-
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MK-8507
|
Reverse Transcriptase
HIV
|
Infection
|
|
Ulonivirine (MK-8507) is an orally active non-nucleoside reverse transcriptase inhibitor with high antiviral activity. Ulonivirine can be used for the research of HIV-1 infection .
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-
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- HY-W325699
-
|
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HIV
Reverse Transcriptase
|
Infection
|
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HIV-1 inhibitor-48 (compound 13o) is a novel non-nucleoside reverse transcriptase inhibitor (NNRTI) and exhibits anti-HIV-1 activity .
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-
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- HY-15352
-
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DPC 083
|
Reverse Transcriptase
HIV
|
Infection
|
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BMS 561390 (DPC 083) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains .
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-
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- HY-14266S
-
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TMC120-d11; R147681-d11
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
|
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
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-
-
- HY-150769
-
|
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HIV
|
Inflammation/Immunology
|
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ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS .
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- HY-106958
-
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HBY 097
|
HIV
Reverse Transcriptase
|
Infection
|
|
Talviraline is a non-nucleoside reverse transcriptase (NNRT) inhibitor that is primarily used to inhibit the replication of human immunodeficiency virus type 1 (HIV-1). Talviraline inhibits the viral replication process by binding to a specific site of HIV-1 reverse transcriptase (RT). Talviraline can be used to study the potential countermeasures and safety of HIV-1 infection .
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- HY-156599
-
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HIV
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Infection
|
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Bavtavirine is a potent non-nucleoside reverse transcriptase inhibitors (NNRTIs). Bavtavirine is part of highly active antitiretroviral therapy (HAART) treatment regimen. Bavtavirine can be used for HIV disease research .
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-
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- HY-90005R
-
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R165335 (Standard); TMC125 (Standard)
|
Reverse Transcriptase
HIV
|
Infection
|
|
Etravirine (Standard) is the analytical standard of Etravirine. This product is intended for research and analytical applications. Etravirine (R165335; TMC125) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
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- HY-10570S
-
-
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- HY-153225
-
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HIV
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Infection
|
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PYR01 is a potent HIV-1 nonnucleoside reverse transcriptase inhibitor. PYR01 is an also targeted activator of cell kill molecules eliminate cells expressing HIV-1 .
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-
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- HY-163110
-
|
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HIV
Reverse Transcriptase
|
Infection
|
|
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .
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-
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- HY-162461
-
|
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Reverse Transcriptase
HIV
|
Infection
|
|
HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
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-
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- HY-10570R
-
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BI-RG 587 (Standard); NSC 641530 (Standard); NVP (Standard)
|
HIV
Reverse Transcriptase
Parasite
|
Infection
Cancer
|
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Nevirapine (Standard) is the analytical standard of Nevirapine. This product is intended for research and analytical applications. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM .
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- HY-152160
-
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HIV
Reverse Transcriptase
|
Infection
|
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HIV-1 invistor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (RT) (IC50=50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains .
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- HY-126900
-
|
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Others
|
Others
|
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HI-253 is a non-nucleoside inhibitor of HIV-1 reverse transcriptase that has demonstrated greater activity than multiple anti-HIV compounds against both resistant and sensitive HIV-1 strains.
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-
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- HY-121611
-
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HIV
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Inflammation/Immunology
|
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HI-236 is a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase.?
HI-236 inhibits HIV activity (wild type HTLVIIB IC50p24 < 0.001 μM) .
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-
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- HY-19378
-
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PC 815
|
HIV
|
Infection
|
|
MIV-150 is a nonnucleoside reverse transcriptase (NNRT) inhibitor, blocking HIV-1 and HIV-2 infections, with an EC50<1 nM against HIV-1/HIV-2MN.
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-
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- HY-118740
-
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HIV
|
Infection
|
|
L-708906 is a potent human immunodeficiency virus type 1 (HIV-1) inhibitor with an IC50 value of 12 μM. L-708906 inhibits HIV strains resistant to nonnucleoside or nucleoside reverse transcriptase inhibitors .
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-
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- HY-105249
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
RDEA 806 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits potent in vitro inhibitory activity against both wild-type HIV-1 (EC50 = 3.05 nM) and NNRTI-resistant HIV-1 .
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-
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- HY-152233
-
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HIV
|
Infection
|
|
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 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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-
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- HY-10571
-
|
U 90152; BHAP-U 90152
|
HIV
Reverse Transcriptase
|
Infection
|
|
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs .
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-
-
- HY-10571A
-
|
U 90152 mesylate; BHAP-U 90152 mesylate
|
HIV
Reverse Transcriptase
|
Infection
|
|
Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26?μM) over DNA polymerase?α?(IC50=440 μM) and polymerase?δ (IC50>550?μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs .
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-
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- HY-16767S1
-
|
MK-1439-13C,d3
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
|
Infection
|
|
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
|
-
-
- HY-10570S1
-
-
-
- HY-168189
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-76 (compound 9t-2) is a non-nucleoside reverse transcriptase inhibitor of HIV-1. HIV-1 inhibitor-76 can be used in anti-HIV research .
|
-
-
- HY-147370
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-46 (compound 13d) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor with an EC50 value of 1.425 μM. HIV-1 inhibitor-46 can be used for the research of AIDS .
|
-
- HY-132291
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM .
|
-
- HY-13053
-
|
Ro-0335
|
Reverse Transcriptase
|
Cancer
|
|
RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates .
|
-
- HY-14361
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
MK-4965 is a nonnucleoside reverse transcriptase inhibitor (NNRTI). MK-4965 displays excellent activities against not only HIV-1 wild-type (WT) virus but also against a broad panel of NNRTI-resistant viruses and can be used for the research of HIV-1 infection .
|
-
- HY-15351
-
|
NSC 675186
|
HIV
|
Infection
|
|
UC-781 (NSC 675186) is a highly potent and selective nonnucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an IC50 value of 5 nM. UC-781 is stable under low PH or various temperatures conditions. UC-781 has antiviral activity and resistance .
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-
- HY-149928
-
|
|
HIV
|
Infection
|
|
NNRTIs-IN-1 is a potent non-nucleoside reverse transcriptase inhibitor featuring significantly anti-resistance efficacy. NNRTIs-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRTIs-IN-1 displays favorable pharmacokinetic properties .
|
-
- HY-15353
-
|
MKC-442
|
HIV
|
Infection
Inflammation/Immunology
|
|
Emivirine (MKC-442) is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) with Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively. Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity .
|
-
- HY-14891
-
|
GSK2248761; FDV
|
HIV
Reverse Transcriptase
|
Infection
|
|
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates .
|
-
- HY-146364
-
|
|
HIV
|
Infection
|
|
CI-39 is an antiviral natural product. CI-39 is an NNRTI (non-nucleoside reverse transcriptase inhibit) antiviral agent with an EC50 of 3.40 µM and an CC50 of >30 µM for wild type HIV-1. CI-39 inhibits HIV-1 RT DNA polymerase and ribonuclease H activitiessup .
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-
- HY-147904
-
|
|
HIV
|
Infection
|
|
HIV-IN-5 (compound 5r) is a potent HIV-1 inhibitor, with an IC50 of 0.16 μM. HIV-IN-5 shows inhibition of HIV DNA-dependent DNA polymerization activity, with an IC50 of 2.18 μM. HIV-IN-5 can bind to NNIBP (NNRTIs (non-nucleoside reverse transcriptase inhibitors) binding pocket) .
|
-
- HY-10572A
-
|
(R)-DMP 266; (R)-EFV; (R)-L-743726
|
Reverse Transcriptase
|
Infection
|
|
(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
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-
- HY-10574
-
|
R278474; TMC278; DB08864
|
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
|
-
- HY-10574A
-
|
TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride
|
SARS-CoV
MMP
|
Infection
|
|
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
|
-
- HY-149991
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-56 (compound 12126065) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-56 has antiviral activity against wild-type HIV-1 in TZM cells with an EC50 value of 0.24 nM. HIV-1 inhibitor-56 penetrates the blood-brain barrier .
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-
- HY-123330
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
GW695634 is an orally active prodrug of GW678248. GW695634 undergoes amidolysis in vivo to release the active ingredient GW678248, thereby inhibiting viral replication. GW678248 is a non-nucleoside reverse transcriptase inhibitor (NNRTi) with potent antiviral activity against Efavirenz (HY-10572)-resistant and Nevirapine (HY-10570)-resistant HIV and AIDS viruses .
|
-
- HY-167746
-
|
|
Others
|
Infection
|
|
Nevirapine quinone methide is an active metabolite of Nevirapine, serving as a non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infection and AIDS. Nevirapine quinone methide is associated with severe skin and liver injuries due to its metabolic activation pathways. Nevirapine quinone methide has been shown to inhibit CYP3A4, which could contribute to its hepatic toxicity.
|
-
- HY-144112
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC50 of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1 resistant strains, with EC50 values of 2.85-18.0 nM .
|
-
- HY-147841
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
|
-
- HY-151933
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
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-
- HY-14266A
-
|
|
Apoptosis
Reverse Transcriptase
Autophagy
HIV
|
Infection
|
|
Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1 .
|
-
- HY-10574S
-
|
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
|
-
- HY-146746
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively[1].
|
-
- HY-144113
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-14 (compound 14b) is a highly potent and broad-spectrum HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor with an EC50 of 0.14 μM for HIV-1 RT. HIV-1 inhibitor-14 has inhibitory activity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM .
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- HY-146018
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HIV
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Infection
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HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability .
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- HY-148642
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12-hydroxy-NVP; 12-OH-NVP
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Drug Metabolite
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Infection
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12-Hydroxynevirapine (12-hydroxy-NVP; 12-OH-NVP) is a major oxidative metabolite of Nevirapine (HY-10570). Nevirapine is a non-nucleoside reverse transcriptase inhibitor indicated for the HIV-1 infections. Nevirapine causes idiosyncratic hepatotoxicity and mild-to-severe skin rashes. 12-Hydroxynevirapine, a non-reactive metabolite, can be bioactivated by sulphotransferases (SULTs) in the liver and skin, yielding the reactive species 12-Sulphoxy-nevirapine .
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- HY-10574AR
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SARS-CoV
MMP
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Infection
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Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
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- HY-147807
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HIV
Cytochrome P450
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Infection
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HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC50 of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC50 values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity .
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- HY-117725
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HIV
Reverse Transcriptase
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Infection
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S-2720 is a potent inhibitor of both immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) and HIV-1 replication. The binding sites of S-2720 and the nonnucleoside compounds overlap. The small pocket in the p66 subunit-BI-RG-587 (HY-10570) complex is most likely the target of S-2720. S-2720 is a quinoxaline derivative, which is promising for research of HIV-1 infection .
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- HY-146017
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HIV
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Infection
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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)
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- HY-146015
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HIV
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Infection
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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) .
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- HY-15350
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LY 300046 hydrochloride
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Reverse Transcriptase
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Others
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Trovirdine hydrochloride, a phenethylthiazolylthiourea (PETT) derivative, is an HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI). A novel computer model of the RT/NNI binding pocket revealed spatial gaps around Trovirdine hydrochloride's pyridyl ring. Docking studies suggested that replacing this planar ring with a nonplanar piperidinyl or piperazinyl ring could better occupy the binding pocket, enhancing anti-HIV activity. Synthesized heterocyclic compounds based on this modification demonstrated greater potency than Trovirdine hydrochloride, effectively inhibiting HIV replication at nanomolar concentrations without cytotoxicity in infected peripheral blood mononuclear cells .
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- HY-162720
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HIV
Potassium Channel
Reverse Transcriptase
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Infection
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NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
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- HY-149866
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Cytochrome P450
HIV
Reverse Transcriptase
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Infection
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HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch .
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- HY-152161
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HIV
Reverse Transcriptase
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Infection
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HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
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- HY-146365
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HIV
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Infection
Inflammation/Immunology
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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 .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-90005S
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Etravirine-d4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
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- HY-10570S
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Nevirapine-d4 is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].
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- HY-132508S
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Etravirine-d8 is the deuterium labeled Etravirine. Etravirine (R165335) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV[1][2].
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- HY-14266S
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Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
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- HY-16767S1
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Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
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- HY-10570S1
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Nevirapine-d3 (BI-RG 587-d3) is the deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM[1].
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- HY-10574S
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Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
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| Cat. No. |
Product Name |
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Classification |
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- HY-152233
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Azide
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Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 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-167690
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Alkynes
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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