NNRT-IN-1 

NNRTIs-IN-1 is a potent non-nucleoside reverse transcriptase inhibitor featuring significantly anti-resistance efficacy. NNRTIs-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC₅₀s in the nanomolar range. NNRTIs-IN-1 displays favorable pharmacokinetic properties^[1].

NNRTIs-IN-1 (compound 8r) inhibits the wild-type HIV-1 (EC₅₀=2.3 nM) and five mutant strains, K103N (EC₅₀=8 nM), E138K (EC₅₀=6 nM), double-digit potency against L100I (EC₅₀=13 nM), Y181C (EC₅₀=29 nM), and Y188L (EC₅₀=52 nM)^[1].
NNRTIs-IN-1 shows no apparent inhibitory effect on CYP1A2, CYP2D6, CYP3A4-T, and CYP3A4-M with IC₅₀ values over 50 μM, and exhibits extremely weak activity toward RPV-sensitive CYP2C9 and CYP2C19 subtypes (IC₅₀=18.5 and 23.6 μM)^[1].
NNRTIs-IN-1 displays very weak inhibition of hERG (IC₅₀>40 μM)^[1].

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

NNRTIs-IN-1 (1 mg/kg; i.v.) exhibits a favorable half-life of 3.66 h and a mean residence time (MRT) of 3.75 h, and the maximal concentration (C_max) is up to 431 ng/mL^[1].
NNRTIs-IN-1 (5 mg/kg; p.o.) exhibits a half-life of 5.18 h, a MRT of 5.21 h, a C_max value of 616 ng/mL, and the oral bioavailability (F) of 31.19%^[1].
NNRTIs-IN-1 (p.o.) is well tolerated at a dose of 2 g/kg^[1].

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

490.51

C₂₈H₂₂N₆O₃

2925364-09-4

CONC(C1=C(N=C(N=C1)NC2=CC=C(C=C2)C#N)OC3=C(C=C(C=C3C)C4=CC=C(C=C4)C#N)C)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sang YL, et, al. Fragment Hopping-Based Design of Novel Biphenyl-DAPY Derivatives as Potent Non-Nucleoside Reverse Transcriptase Inhibitors Featuring Significantly Improved Anti-Resistance Efficacy. J Med Chem. 2023 Apr 13;66(7):4755-4767.  [Content Brief]