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。

HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV?1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC 50 =4.44~54.5 nM) against various HIV?1 strains. The IC 50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.

Solid

HIV-1 (WT) 0.081 μM (IC50)

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

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Wang Z, et al. Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;1

In Vitro: DMSO : 50 mg/mL (113.76 mM; Need ultrasonic)配制储备液