NYX-PCSK9i

Chemical Structure : NYX-PCSK9i

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货号: PC-49372Not For Human Use, Lab Use Only.

NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of PCSK9, inhibits PCSK9-LDLR interaction with IC50 of 323 nM in in vitro biochemical binding assays.

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生物&药学活性

NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of PCSK9, inhibits PCSK9-LDLR interaction with IC50 of 323 nM in in vitro biochemical binding assays.
NYX-PCSK9i (30 and 50 mg/kg) demonstrates significant cholesterol-lowering properties in APOE*3-Leiden.CETP hyperlipidemic mice, significantly reduces plasma total cholesterol and elevates plasma total PCSK9 levels in a dose-dependent fashion.
NYX-PCSK9i enhances the efficacy of atorvastatin in lowering plasma total cholesterol levels in female APOE*3-Leiden.CETP mice.
NYX-PCSK9i modulates the hepatic transcriptional activity of specific genes involved in cholesterol metabolism (Pcsk9, Ldlr, Srebf2 and Mttp).
NYX-PCSK9i depletes hepatic cholesteryl ester levels and promotes faecal cholesterol elimination in female APOE*3-Leiden.CETP mice.

物理化学性质&存储条件

分子量	466.589
分子式	C28H30N6O
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)-N-(3-((3-aminopiperidin-1-yl)methyl)-5-(4-methyl-1H-imidazol-1-yl)phenyl)-4-phenylpicolinamide

参考文献

1. Suchowerska AK, et al. J Lipid Res. 2022 Oct 6:100293.

NYX-PCSK9i

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物理化学性质&存储条件

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NYX-PCSK9i

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