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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
20 Results for "
Y181
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "Y181" in MCE Product Catalog:
14
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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 .
Cat. No.: HY-16767S1
Synonyms: MK-1439-13C,d3
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-N16422
CAS No.: 159121-98-9
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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-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-150599
CAS No.: 2493426-43-8
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HIV-1 inhibitor-43 is a potent HIV-1 inhibitor with an EC50 of 21.3 nM, 6.2 nM, < 0.7 nM and < 0.7 nM for Y188L, K103N-Y181C, K103N and Y181C, respectively. HIV-1 inhibitor-43 can reduce HIV-1 RNA and protein p24 expression .
Cat. No.: HY-116528
CAS No.: 149950-61-8
GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively .
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 .
Cat. No.: HY-172408
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NNRT-IN-6 (Compound 13a) is the non-nucleoside reverse transcriptase inhibitor (NNRT) for HIV-1 reverse transcriptase (HIV-1 RT) with IC50 of 0.41 μM. NNRT-IN-6 inhibits HIV-1 wildtype and mutant strains L100I, K103N, Y181C, Y188L, E138K, F227L/V106A and RES056 with EC50 of 6.2-250 nM .
Cat. No.: HY-144122
CAS No.: 2757182-99-1
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
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-144123
CAS No.: 2719675-72-4
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
Cat. No.: HY-175491
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HIV-1-IN-85 is an orally active HIV-1 inhibitor (IC50 = 72 nM). HIV-1-IN-85 exhibits strong inhibitory activity against wild-type (WT) HIV-1 and NNRTI-resistant single mutant strains (L100I, K103N, Y181C, Y188L, E138K) and moderate efficacy against double mutant strains (F227L+V106A, RES056). HIV-1-IN-85 shows good in vivo safety in ICR mice. HIV-1-IN-85 can be used for the study of HIV-1 infection .
Cat. No.: HY-146019A
CAS No.: 2475658-74-1
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 .
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-182474
CAS No.: 352548-47-1
Synonyms: Indolopyridone-1
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INDOPY-1 (Indolopyridone-1) is a selective, reversible, and competitive HIV-1 reverse transcriptase inhibitor. INDOPY-1 reversibly binds to the active site of reverse transcriptase. INDOPY-1 inhibits DNA synthesis. INDOPY-1 exhibits antiviral activity against various retroviruses, including HIV-1 IIIB, HIV-1 HXB2 K103N Y181C, HIV-2 ROD, and SIV Mac251. INDOPY-1 can be used in the research of immunodeficiency virus infection .
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-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 .
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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
