PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.
Gadoleic acid is a monounsaturated fatty acid.1,2It inhibits the dsDNA binding activity of p53 when used at a concentration of 1.2 nM.1Hepatic levels of gadoleic acid are reduced in rats fed a high-fat or a high-fat high-cholesterol diet and increased in rats fed a high-cholesterol diet.2 1.Iijima, H., Kasai, N., Chiku, H., et al.The inhibitory action of long-chain fatty acids on the DNA binding activity of p53Lipids41(6)521-527(2006) 2.Serviddio, G., Bellanti, F., Villani, R., et al.Effects of dietary fatty acids and cholesterol excess on liver injury: A lipidomic approachRedox Biol.9296-305(2016)
AT-9010, a triphosphate derivative of AT-527, exhibits strong inhibitory activity against NiRAN, a crucial viral replication function. This compound effectively suppresses the replication of SARS-CoV-2.
AT-9010 tetrasodium is a triphosphate active metabolite derived from AT-527. It acts as a potent inhibitor of NiRAN, a crucial function for viral replication. Furthermore, AT-9010 tetrasodium demonstrates its ability to effectively inhibit the replication of SARS-CoV-2.
AT-9010 triethylamine, a triphosphate active metabolite of AT-527, is a potent inhibitor of the NiRAN enzyme, which is essential for viral replication. It effectively inhibits SARS-CoV-2 replication.