NNRT-IN-10 

NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC₅₀ values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1^[1].

NNRT-IN-10 (48 h) (Compound 5i3) with improved resistance profiles and no apparent cytotoxicity, with EC₅₀ values of 1.16 nM (HIV-1, WT), 2.64 nM (P1579), 12.5 nM (P5375), 3.70 nM (P1833) and 18.3 (P5735), and EC₅₀ = 11.1 nM for the Rilpivirine (HY-10574)-resistant strain GH9, respectively in TZM-bl cells^[1].
NNRT-IN-10 (5 days) suppresses the replication of HIV-1 IIIB very effectively at single-digit nanomolar levels (EC₅₀ = 1.4 nM) in MT-4 cells^[1].
NNRT-IN-10 shows only faint inhibition of CYP1A2 (IC₅₀ = 56.6 μM), CYP2C9 (IC₅₀ = 6.76 μM), CYP2C19 (IC₅₀ = 8.47 μM), and CYP2D6 (IC₅₀ = 12.7 μM)^[1].
NNRT-IN-10(24 h) displays potassium channel inhibitory activity with an IC₅₀ value of 1.48 μM in CHO-hERG cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NNRT-IN-10 (Compound 5i3) (800 mg/kg, p.o., single dose) shows good tolerance and no acute toxicity to mice. ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

568.69

C₃₁H₃₂N₆O₃S

2459751-62-1

CC1=CC(/C=C/C#N)=CC(C)=C1OC2=C(C=CC=N3)C3=NC(NC4CCN(CC5=CC=C(S(C)(=O)=O)C=C5)CC4)=N2

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• [1]. Li W, et al. A nanoparticle-encapsulated non-nucleoside reverse-transcriptase inhibitor with enhanced anti-HIV-1 activity and prolonged circulation time in plasma. Curr Pharm Des. 2015;21(7):925-35.  [Content Brief]