Search Result
Results for "
non-nucleoside reverse transcriptase
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-W325699
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-48 (compound 13o) is a novel non-nucleoside reverse transcriptase inhibitor (NNRTI) and exhibits anti-HIV-1 activity .
|
-
-
- 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-15379
-
|
HIV
|
Infection
|
Atevirdine is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Atevirdine inhibits non-nucleoside reverse transcriptase that leads to viral multiplication .
|
-
-
- HY-10574
-
Rilpivirine
Maximum Cited Publications
9 Publications Verification
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-117477
-
|
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 .
|
-
-
- HY-146031
-
|
HIV
|
Infection
|
A3N19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with an EC50 of 3.28 nM against HIV-1 IIIB .
|
-
-
- HY-107001
-
(S)-DPC 961; DMP 961
|
HIV
Reverse Transcriptase
|
Infection
|
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 .
|
-
-
- 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-152233
-
|
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.
|
-
-
- HY-10572A
-
(R)-DMP 266; (R)-EFV; (R)-L-743726
|
Reverse Transcriptase
|
Infection
Metabolic Disease
|
(R)-Efavirenz 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 .
|
-
-
- 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-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 .
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-
-
- HY-148248
-
|
HIV
|
Infection
|
BI-2540 is a HIV non-nucleoside reverse transcriptase (NNRT) inhibitor .
|
-
-
- HY-90005
-
R165335; TMC125
|
Reverse Transcriptase
HIV
|
Infection
|
Etravirine (R165335; TMC125) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
|
-
-
- HY-148642
-
12-hydroxy-NVP; 12-OH-NVP
|
Drug Metabolite
|
Infection
|
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 .
|
-
-
- HY-10570
-
-
-
- HY-90005S
-
TMC-125 d4; R-165335 d4
|
Reverse Transcriptase
HIV
|
Infection
|
Etravirine-d4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
|
-
-
- HY-149338
-
|
HIV Protease
|
Infection
|
NNRT-IN-3 (compound 8) is an HIV-1 non-nucleoside reverse transcriptase inhibitor (EC50=0.01 μM) .
|
-
-
- HY-139158
-
|
HIV
|
Infection
|
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 .
|
-
-
- HY-132508S
-
-
-
- HY-15352
-
DPC 083
|
Reverse Transcriptase
HIV
|
Infection
|
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 .
|
-
-
- HY-147411
-
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 .
|
-
-
- HY-15355
-
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 .
|
-
-
- HY-118423
-
IQP-0410
|
HIV
|
Inflammation/Immunology
|
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 .
|
-
-
- HY-156599
-
|
HIV
|
Infection
|
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 .
|
-
-
- HY-90005R
-
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.
|
-
-
- HY-14294
-
S-1153
|
Reverse Transcriptase
|
Infection
|
Capravirine 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 .
|
-
-
- HY-10570S
-
-
-
- HY-10570R
-
BI-RG 587 (Standard); NSC 641530 (Standard); NVP (Standard)
|
HIV
Reverse Transcriptase
Parasite
|
Infection
Cancer
|
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 .
|
-
-
- HY-162461
-
|
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 .
|
-
-
- HY-121611
-
|
HIV
|
Inflammation/Immunology
|
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) .
|
-
-
- HY-106958
-
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 .
|
-
-
- HY-150769
-
|
HIV
|
Inflammation/Immunology
|
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 .
|
-
-
- HY-152161
-
|
HIV
Reverse Transcriptase
|
Infection
|
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) .
|
-
-
- HY-163110
-
|
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 .
|
-
-
- 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 of 3.05 nM) and NNRTI-resistant HIV-1 .
|
-
-
- HY-10570S1
-
-
-
- HY-152160
-
|
HIV
Reverse Transcriptase
|
Infection
|
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 .
|
-
-
- 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-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 .
|
-
-
- 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 .
|
-
-
- 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 .
|
-
-
- 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-118632
-
|
Reverse Transcriptase
HIV
|
Infection
|
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 .
|
-
-
- 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 .
|
-
-
- 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-130241
-
|
HIV
|
Infection
|
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 .
|
-
-
- 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 .
|
-
- HY-142073
-
DHCal A; NSC 678323
|
Reverse Transcriptase
HIV
|
Infection
|
(+)-Dihydrocalanolide A (DHCal A; NSC 678323) is an orally active nonnucleoside inhibitor of Reverse Transcriptase. (+)-Dihydrocalanolide A can be used to HIV infection research .
|
-
- HY-14266
-
TMC120; R147681
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
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 .
|
-
- HY-16767
-
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 .
|
-
- 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 .
|
-
- 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-146018
-
|
HIV
|
Infection
|
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 .
|
-
- HY-129667
-
|
Reverse Transcriptase
|
Infection
|
BM 21.1298 is a selective and high specific nonnucleoside immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) inhibitor with antiviral activity .
|
-
- HY-147807
-
|
HIV
Cytochrome P450
|
Infection
|
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 .
|
-
- HY-14266S
-
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].
|
-
- HY-153225
-
|
HIV
|
Infection
|
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 .
|
-
- HY-146017
-
|
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)
|
-
- HY-15350
-
LY 300046 hydrochloride
|
Reverse Transcriptase
|
Others
|
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 .
|
-
- HY-146015
-
|
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) .
|
-
- HY-162720
-
|
HIV
Potassium Channel
Reverse Transcriptase
|
Infection
|
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) .
|
-
- HY-19378
-
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.
|
-
- HY-118740
-
|
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 .
|
-
- 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-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-19509
-
|
Reverse Transcriptase
HIV
|
Infection
|
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 .
|
-
- HY-14361
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HIV
Reverse Transcriptase
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Infection
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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 .
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- HY-15351
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NSC 675186
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HIV
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Infection
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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-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-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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- 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 human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) activity 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 also 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-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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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-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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- 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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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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