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LSN3353871

Chemical Structure : LSN3353871

CAS No.: 2565657-20-5

LSN3353871 (LSN-3353871)

货号: 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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 255.74
分子式 C13H18ClNO2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-3-Phenyl-2-((R)-pyrrolidin-3-yl)propanoic acid hydrochloride

参考文献

1. Nuria Diaz, et al. Nature. 2024 May;629(8013):945-950.

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