Catalog No.: PC-24907Not For Human Use, Lab Use Only.
LSN3353871 is a potent small-molecule apolipoprotein(a) (apo(a)) binder and inhibitor of Lipoprotein(a) (Lp(a)) formation, disrupts the formation of Lp(a) with IC50 of 1.69 uM in in vitro Lp(a) assembly assays.
LSN3353871 is a potent small-molecule apolipoprotein(a) (apo(a)) binder and inhibitor of Lipoprotein(a) (Lp(a)) formation, disrupts the formation of Lp(a) with IC50 of 1.69 uM in in vitro Lp(a) assembly assays. LSN3353871 binds to KIV8, KIV7-8 and KIV5-8 with Kd values of 756 nM, 605 nM and 423 nM, respectively. Oral administration of LSN3353871 to mice expressing human Lp(a) resulted in dose-dependent increases in the circulating levels of LSN3353871 and dose-dependent decreases of up to 78% in the levels of Lp(a), with a median effective dose (ED50) of 14 mg/kg twice daily (BID) within five days of dosing. LSN3353871 (20 mg/kg, BID for two weeks) resulted in a decrease of up to 40% in the levels of Lp(a) in cynomolgus monkeys.
