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.

NNRT-IN-9 (Compound EG28) is a non-nucleoside reverse transcriptase inhibitor (NNRT). It demonstrates strong antiviral and resistance-fighting activity against wild-type (WT) and various clinically relevant mutant strains (E138K and K103N + Y181C) of HIV-1, with EC50 values of 55 nM, 67 nM, and 3910 nM, respectively. NNRT-IN-9 is applicable in acquired immunodeficiency syndrome (AIDS) research.

DPC 684 is a potent and selective HIV-1 protease inhibitor with an IC90 of 5.7-40 nM and a Ki of 0.021 nM. It competitively inhibits HIV-1 protease, preventing viral polyprotein cleavage. Compared to cellular proteases, DPC 684 shows high selectivity for retroviral proteases. The compound exhibits low protein binding and offers broad-spectrum inhibition against various wild-type and mutant HIV-1 proteases, with an IC90 of 1.9-6.3 nM. DPC 684 is significant for HIV research.

HIV-1-IN-83 (Compound 18E) is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1. It demonstrates an IC50 of 0.45 μM against wild-type HIV-1 reverse transcriptase. HIV-1-IN-83 exhibits potent antiviral activity against both wild-type and mutant HIV-1 strains and enhances drug resistance in Y188L and RES056 mutants. The compound is non-toxic up to a concentration of 11.088 μM.

HIV-1-IN-85 is an orally active HIV-1 inhibitor with an IC50 of 72 nM. It exhibits potent inhibitory activity against wild-type (WT) HIV-1 and single mutant strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs), such as L100I, K103N, Y181C, Y188L, and E138K. Additionally, it shows moderate inhibitory activity against double mutant strains (F227L+V106A, RES056). In ICR mice, HIV-1-IN-85 demonstrates good in vivo safety and is suitable for research on HIV-1 infection.

NNRT-IN-11 (14l) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor, exhibiting EC50 values ranging from 6.50 to 52.9 nM against both wild-type (WT) and a range of HIV-1 mutant strains. NNRT-IN-11 demonstrates antiviral properties.

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.