NNRT-IN-1,2925364-09-4

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NNRTIs-IN-1

CAS No. : 2925364-09-4

MCE 国际站：NNRTIs-IN-1

产品活性：NNRTIs-IN-1 是一种有效的非核苷逆转录酶抑制剂，具有显着的抗耐药性。NNRTIs-IN-1 抑制野生型 HIV-1 和五种突变株，EC₅₀ 值在纳摩尔范围。NNRTIs-IN-1 显示出良好的药代动力学特性。

研究领域：Anti-infection

作用靶点：HIV

In Vitro: 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).
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).
NNRTIs-IN-1 displays very weak inhibition of hERG (IC₅₀>40 μM).

In Vivo: 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.
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%.
NNRTIs-IN-1 (p.o.) is well tolerated at a dose of 2 g/kg.

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