U 81749

U 81749 competitively inhibits recombinant HIV-1 protease in vitro with a K_i value of 70 nM, while its inhibitory potency against human renin is over 100-fold lower^[1].
U 81749 (0.001-1 μM; 3-4 days) inhibits HIV-1 replication in acutely infected human peripheral blood lymphocytes, with an IC₅₀ of 0.1 to 1 μM, and reduces viral p24 and RNA levels in a concentration-dependent manner^[1].
U 81749 (2.5-10 μM; 24 h) inhibits the processing of HIV-1 gag polyprotein p55 into mature proteins p24 and p17 in vVK-1-infected CV-1 cells in vitro in a concentration-dependent manner^[1].
U 81749 (10 μM; 16 h) blocks the maturation of HIV-1-like particles released from vVK-1-infected CV-1 cells, resulting in particles composed primarily of the gag precursors p55 and p46 instead of the mature p24^[1].
The inhibition of HIV-1-like particle maturation mediated by U 81749 (10 μM; initial treatment for 16 h, post-recovery incubation for 1-2 h) is partially reversible, as removal of the drug allows processing of the gag precursor into mature p24, confirming that the drug acts directly on the viral protease within the particles^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.