wild-type hiv-1

TMC310911 is an effective and orally active HIV type-1 protease inhibitor (EC50: ranged from 2.2 nM to 14.2 nM for wild-type HIV-1). TMC310911 has effective activity against a wide spectrum of recombinant HIV-1 isolates.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

DPC-681 is a potent and selective HIV protease inhibitor with IC90 values ranging from 4 to 40 nM for wild-type HIV-1.

HIV-1 inhibitor-54 is a potent inhibitor of WT HIV-1 (strain IIIB) in MT-4 cells, demonstrating anti-HIV activity with an EC50 of 32 nM. [HIV-1 inhibitor-54 can be used to study viral infections.]

Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.

HIV-1inhibitor-78 (compound 15f) is a potent and broad-spectrum non-nucleoside reverse transcriptase inhibitor, with an EC50 value of 3 nM against wild-type HIV-1. It is useful for research on HIV infections.

NNRT-IN-6 (Compound 13a) is a non-nucleoside reverse transcriptase inhibitor (NNRT) used to inhibit HIV-1 reverse transcriptase (HIV-1RT), with an IC50 of 0.41 μM. It effectively suppresses both wild-type HIV-1 and mutants L100I, K103N, Y181C, Y188L, E138K, F227L V106A, and RES056, with an EC50 range of 6.2-250 nM.

HIV-1protease-IN-13 (compound 18d) is a potent inhibitor of HIV-1 protease (HIV-1protease) with an IC50 value of 0.54 nM. Additionally, HIV-1protease-IN-13 demonstrates effective activity against both HIV-1DRVRS (DRV resistant mutation) and HIV-1NL4_3 variants (wild-type).

HIV-1inhibitor-66 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits inhibitory activity against wild-type HIV-1 reverse transcriptase (HIV-1 reverse transcriptase) with an IC50 of 40 nM.

NNRT-IN-4 (Compound 10p) is an inhibitor of non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1RT. It exhibits antiviral activity against both wild-type and mutant strains of HIV-1, with an EC50 ranging from 6 to 63 nM. NNRT-IN-4 shows weak inhibitory activity on hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). In mice, NNRT-IN-4 demonstrates good tolerance and safety at 2 g/kg.

Rilpivirine HCl (Rilpivirine hydrochloride) is a selective and potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with antiviral activity that inhibits the HIV virus and can be used in the study of HIV infections.

AIC-292 is a potent reverse transcriptase inhibitor with well tolerated in different cell lines. In addition, activity of AIC292 could be demonstrated against a broad panel of wild-type HIV-1 group. AIC292 also retained activity against viruses harboring

DPC-082 is a reverse transcriptase inhibitor. DPC-082 exhibits low-nanomolar potency toward wild-type virus, L100I and K103N single-mutation variants, and multiplies amino acid-substituted HIV type 1 mutants.

Tenofovir exalidex (CMX 157) is a lipid-conjugated acyclic nucleotide analog of Tenofovir, demonstrating efficacy against wild-type and antiretroviral-resistant HIV strains, including those resistant to multiple nucleoside/nucleotide analogs. It effectively inhibits all major HIV-1 and HIV-2 subtypes in fresh human PBMCs, as well as all evaluated HIV-1 strains in monocyte-derived macrophages, displaying EC50 values between 0.2 and 7.2 nM. Oral administration of CMX157 shows no apparent toxicity. Additionally, Tenofovir exalidex exhibits antiviral properties against HBV.

HIV-1 inhibitor-9 exhibits potent inhibition activity at low nanomolar concentrations against both the wild-type (WT) HIV-1 strain and multiple strains that have developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs).

HIV-1 inhibitor-16 (compound 7a) is a potent HIV-1 inhibitor with an EC50 of 1.3 nM against wild-type HIV-1, and exhibits 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, respectively. It demonstrates good solubility, hepatic microsomal stability, and lacks significant CYP enzyme inhibitory activity or acute toxicity.

HIV-1 inhibitor-44 (compound 11l) is an HIV-1 reverse transcriptase inhibitor with activity against wild-type HIV-1 strains (EC50: 0.209 μM).

HIV-1 inhibitor-24 (compound S-12a) is a potent inhibitor of HIV-1 reverse transcription (HIV-1 RT) with an IC50 of 9.5 nM. It exhibits a high antiviral effect on wild-type HIV-1, showing an EC50 value of 1.6 nM and low cytotoxicity (CC50 on MT-4 cells). HIV-1 inhibitor-24 was well tolerated in mice at a dose of 2 g/kg and demonstrated a significant cardiovascular safety profile.

HIV-1 inhibitor-25 (compound R-12a) is a potent inhibitor of HIV-1 reverse transcription (HIV-1 RT) with an IC50 of 0.1061 nM. It exhibits a high antiviral effect against wild-type HIV-1 (EC50: 13.6 nM) and demonstrates low cytotoxicity (to MT). It also inhibits HIV-1 mutants (L100I, K103 N, Y181C, Y188L, E138K, F227L+V106A) with EC50 values ranging from 0.1961 to 5.8136 μM. HIV-1 inhibitor-25 is useful for studying AIDS.

HIV-1 inhibitor-21 (compound 9b) is a potent inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) with an IC50 of 0.55 μM. It inhibits both wild-type HIV-1 (EC50: 12.7 nM) and mutant virus strain K103N (EC50: 10.4 nM), demonstrating relatively low cytotoxicity (CC50 for MT-4: 10.2 μM).

HIV-1 inhibitor-32 is a potent inhibitor of HIV-1 that acts on wild-type HIV (IC50: 34 nM) and can be used in AIDS research.

HIV-1 inhibitor-28 is a potent and selective HIV-1 inhibitor with EC50=58 nM for wild-type HIV-1, IC50=3.37 μM for wild-type HIV-1 reverse transcription, and relatively low toxicity to MT-4 cells with CC50= 38.6 μM. HIV-1 inhibitor-28 can be used in AIDS research.

HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor with an IC50 of 21 pM and a Ki of 4.7 pM, demonstrating significant antiviral activity against DRV (darunavir) resistant mutants, surpassing its inhibition efficacy against wild-type viruses.

HIV-1 inhibitor-14 is a potent, broad-spectrum inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) (IC50=0.14 μM for HIV-1 RT). HIV-1 inhibitor-14 inhibits both wild-type and drug-resistant HIV-1 strains (EC50: 5.79-28.3 nM).