NNRT-IN-1 

NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC₅₀s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties^[1].

NNRT-IN-1 (compound 8r) 抑制野生型 HIV-1 (EC₅₀=2.3 nM) 和五种突变株：K103N (EC₅₀=8 nM)，E138K (EC₅₀=6 nM)，L100I (EC₅₀=13 nM)，Y181C (EC₅₀=29 nM) 和 Y188L (EC₅₀=52 nM)^[1]。
NNRT-IN-1 对 CYP1A2，CYP2D6，CYP3A4-T 和 CYP3A4-M 没有明显的抑制作用，IC₅₀ 值超过 50 μM，对 RPV 敏感的 CYP2C9 和 CYP2C19 亚型表现出极弱的活性 (IC₅₀=18.5 和 23.6 μM)^[1]。
NNRT-IN-1 对 hERG 表现出非常弱的抑制作用 (IC₅₀>40 μM)^[1]。

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

NNRT-IN-1 (compound 8r) (1 mg/kg; i.v.) 的半衰期为 3.66 h，平均停留时间 (MRT) 为 3.75 h，最大浓度 (C_max) 高达 431 ng/mL^[1]。
NNRT-IN-1 (1 mg/kg; i.v.) 的半衰期为 5.18 h，MRT 为 5.21 h，C_max 为 616 ng/mL，口服生物利用度 (F) 为 31.19%^[1]。
NNRT-IN-1 (p.o.) 在 2 g/kg 的剂量下具有良好的耐受性^[1]。

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

490.51

C₂₈H₂₂N₆O₃

2925364-09-4

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]