hiv-1 inhibitor-15

HIV-1 inhibitor-15 (compound 9d) is a potent, broad-spectrum inhibitor targeting HIV-1, with EC50 values of 1.7 nM against HIV-1 WT, 4 nM against L100I, 2 nM against K103N, 6 nM against Y181C, and 9 nM against E138K. It exhibits high efficacy, favorable solubility, safety profiles, and oral bioavailability [1].

BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains.

GSK3532795 (also known as BMS-955176) is a potent oral second-generation HIV-1 maturation inhibitor (MI) that has advanced to phase IIb clinical trials. This compound exhibits broad coverage against polymorphic viruses (EC50 < 15 nM, covering common polymorphisms representing 96.5% of HIV-1 subtype B) and demonstrates favorable pharmacokinetic properties in preclinical species.

HIV-1 integrase inhibitor 13 (Compound 15) is an inhibitor of HIV-1 integrase, with an IC50 value of 1.8 nM. It can inhibit HIV-1WT and HIV-1T125A, with IC50 values of 21 and 580 nM, respectively.

GSK3532795 is an orally active inhibitor of HIV-1 maturation. GSK3532795 combines broad coverage of polymorphic viruses (EC50: 15 nM toward a panel of common polymorphisms representative of 96.5% HIV-1 subtype B virus) with a favorable pharmacokinetic pro

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

F1, an anti-inflammatory peptide, incorporates the HIV-1 Tat protein transduction domain linked with a 15-amino acid sequence from residues 46-60 of the inhibitor of NF-κB kinase-interacting peptide (IKIP). It effectively blocks LPS-induced phosphorylation of IκB kinase α (IKKα) and IKKβ, along with the nuclear translocation of NF-κB (p65) in mouse peritoneal macrophages at 5 µM concentration. F1, administered at 5 mg/kg in vivo, significantly reduces IL-6, TNF-α, and IL-1β serum levels and enhances survival in a mouse sepsis model induced by LPS.