HIV-1 inhibitor-8,2826996-78-3

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HIV-1 inhibitor-8

CAS No. : 2826996-78-3

MCE 国际站：HIV-1 inhibitor-8

产品活性：HIV-1 inhibitor-8 是一种具有口服活性、低毒和有效的 HIV -1 非核苷逆转录酶抑制剂 (NNRTI)。HIV-1 inhibitor-8 对各种 HIV -1 菌株产生有效的抗病毒活性 (EC₅₀=4.44~54.5 nM)。HIV-1 inhibitor-8 对 WT HIV-1 逆转录酶的 IC₅₀ 为 0.081 μM。

研究领域：Anti-infection

作用靶点：HIV

In Vitro: HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC₅₀=4.44~54.5 nM) against various HIV-1 strains and improves resistance profiles (RF = 0.5~5.6). HIV-1 inhibitor-8 exhibits reduces cytotoxicity (CC₅₀=284 μM) and higher SI values (SI = 5210~63992). HIV-1 inhibitor-8 displays better solubility (sol. =12.8 μg/mL) and no significant inhibition of the main CYP enzymes. HIV-1 inhibitor-8 displays an extremely low hERG inhibition with an IC₅₀ value of 19.84 μM in CHO-hERG cells.

In Vivo: HIV-1 inhibitor-8 (2 mg/kg; i.v.) shows a favorable mean CL, volume of distribution and a long terminal half-life.
HIV-1 inhibitor-8 (20 mg/kg; p.o.) absorption reaches maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time is 2.90 hours.

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