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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
139 Results for "
nonnucleoside reverse transcriptase
" in MedChemExpress (MCE) Product Catalog:
Products (139)
139 Results for "nonnucleoside reverse transcriptase" in MCE Product Catalog:
Cat. No.: HY-174303
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NNRT-IN-9 (Compound EG28) is a non-nucleoside reverse transcriptase (NNRT) inhibitor. NNRT-IN-9 has potent antiviral and anti-resistance activity against wild-type (WT) HIV-1 and various clinically relevant mutations (E138K and K103N + Y181C) with EC50s of 55, 67 and 3910 nM, respectively. NNRT-IN-9 can be used for acquired immune deficiency syndrome (AIDS) research .
Cat. No.: HY-W003486
CAS No.: 57489-77-7
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5,7-Dichloropyrazolo[1,5-a]pyrimidine is a PDE10A inhibitor with a Ki of 24 μM. 5,7-Dichloropyrazolo[1,5-a]pyrimidine serves as a key intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives (HIV-1 non-nucleoside reverse transcriptase inhibitors). 5,7-Dichloropyrazolo[1,5-a]pyrimidine can be used for the research of schizophrenia .
Cat. No.: HY-120055
CAS No.: 343250-05-5
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CP-94707 is an HIV-1 reverse transcriptase (HIV-1 reverse transcriptase) inhibitor, with an IC50 of 4 μM against wild-type and HIV-1 reverse transcriptase Y181I-Y188L double mutant enzymes, and an IC50 of 10 μM against HIV-1 reverse transcriptase K103N mutant enzyme. CP-94707 inhibits the initiation of negative-strand DNA synthesis primed by tRNA Lys-3, as well as the elongation of DNA synthesis mediated by HIV-1 reverse transcriptase. CP-94707 can be used in studies related to HIV infection .
Cat. No.: HY-146017
CAS No.: 2554618-33-4
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)
Cat. No.: HY-175667
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NNRT-IN-12 (compound 19) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor with an IC50 value of 0.107 μM for WT HIV-1 RT. NNRT-IN-12 shows anti-HIV-1 activity with EC50 value of 14.1, 5.03, 7.64, 27.1 nM for L100I, K103N, Y181C, Y188L mutant HIV-1 strains, respectively. NNRT-IN-12 shows cytotoxicity .
Cat. No.: HY-109056A
CAS No.: 867365-40-0
Synonyms: R-1206 sodium
Elsulfavirine sodium (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine sodium also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine sodium and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine sodium is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine sodium exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine sodium is used in studies related to HIV-1 infection and liver cancer .
Cat. No.: HY-146015
CAS No.: 2554620-04-9
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) .
Cat. No.: HY-162720
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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) .
Cat. No.: HY-182916
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NNRT-IN-16, Rilpivirin (HY-10574) analogue, is a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRT-IN-16 inhibits recombinant WT HIV-1 RT with an IC50 of 0.07 μM. NNRT-IN-16 exerts antiviral activity against wild-type and drug-resistant HIV-1 mutants, shows attenuated CYP isoenzyme and hERG inhibition, reduced cytotoxicity, and improved metabolic stability in human liver microsomes. NNRT-IN-16 can be used for the research of HIV-1 infection .
Cat. No.: HY-178031
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HIV-1-IN-87 (Compound 11x) is a dual-site HIV-1 inhibitor targeting the non-nucleoside reverse transcriptase inhibitor binding pocket (NNIBP) and its adjacent site (NNIAS). HIV-1-IN-87 has potent antiviral activities against wild-type and mutant strains (such as L100I, K103N and Y181C) (EC50: 4.1-150 nM). HIV-1-IN-87 can be used for HIV-1 infections like acquired immune deficiency syndrome (AIDS) research .
Cat. No.: HY-19869
CAS No.: 878670-89-4
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VRX-480773 is an efficient non-nucleoside reverse transcriptase inhibitor (NNRTI), used for HIV infection. VRX-480773 has high specificity for HIV-1, with an EC50 for wild-type HIV-1 being 0.14 nM. VRX-480773 does not inhibit HIV-2, HBV or HCV, and has no effect on human DNA polymerase α/β. VRX-480773 retains inhibitory activity against Efavirenz (HY-10572) resistant strains, with EC50s mostly < 1 nM. VRX-480773 can be used for research on AIDS .
Cat. No.: HY-184318
CAS No.: 915407-80-6
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GS-9160 is a HIV-1 integrase strand transfer inhibitor with an IC50 of 28 nM. GS-9160 elevates the level of HIV-1 double long terminal repeat circles and reduces integration junctions. GS-9160 exhibits selective antiviral activity against HIV-1 in cells. GS-9160 can select for integrase mutants E92V and L74M, and shows synergistic activity with other HIV-1 inhibitors. GS-9160 can be used in studies related to HIV-1 infection .
Cat. No.: HY-109056R
CAS No.: 868046-19-9
Synonyms: R-1206 (Standard)
Elsulfavirine (Standard) is the analytical standard of Elsulfavirine (HY-109056). This product is intended for research and analytical applications. Elsulfavirine (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer .
Cat. No.: HY-179348
CAS No.: 3020859-44-0
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DPP9-IN-2 is a selective, potent and orally active inhibitor of Dipeptidyl Peptidase 9 (DPP9 ) with an IC50 of 12.9 nM. DPP9-IN-2 shows a SI of 59 over DPP8, and shows no significant inhibitory activity against related peptidases including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce cancer cells pyroptosis and has weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitor. DPP9-IN-2 can be used for the researches of cance rand infection .
Cat. No.: HY-149866
CAS No.: 3034064-68-8
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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 .
Cat. No.: HY-181034
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NNRT-IN-15 (Compound 16a) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor. NNRT-IN-15 shows an EC50 of 3 nM for WT HIV-1 and inhibits seven mutant strains (L100I, K103N, Y181C, etc.) (EC50 = 8.2-43.4 nM). NNRT-IN-15 has low cytotoxicity against MT-4 cells (CC50 = 196.46 μM). NNRT-IN-15 also inhibit WTHIV-1RT and hERG with IC50 values of 0.7599 μM and 27.455 μM. NNRT-IN-15 can be used for research of HIV-1 infection .
Cat. No.: HY-152161
CAS No.: 2834087-82-8
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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) .
Cat. No.: HY-146365
CAS No.: 2132412-77-0
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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 .
Cat. No.: HY-167690
CAS No.: 1034474-19-5
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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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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
