HIV-1 inhibitor-24

Names

[ CAS No. ]:
2475658-75-2

[ Name ]:
HIV-1 inhibitor-24

Biological Activity

[Description]:

HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV
Research Areas >> Infection

[Target]

HIV-1 (WT):1.6 nM (EC50)


[In Vivo]

HIV-1 inhibitor-24 (2 g/kg; IG; single dosage) is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety[1]. Animal Model: Mice[1] Dosage: 2 g/kg Administration: IG; single dosage Result: Exhibited well tolerance at a dose of 2 g/kg in mice and a significant cardiovascular safety.

[References]

[1]. Chen X, et al. Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. Eur J Med Chem. 2020;202:112549.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H19N5O2

[ Molecular Weight ]:
433.46


Related Compounds