PCSK9-IN-13_product_DataBase

Bioactivity	PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM[1].
Invitro	PCSK9-IN-13(compound 3f) (0.1 or 1 μM) 可剂量依赖性的恢复 HepG2 肝细胞对 LDL 的摄取[1]。
In Vivo	PCSK9-IN-13(compound 3f) (3.28 or 16.4 mg/kg/day, s.c., 14 days) 在雄性 C57BL/6 小鼠中，剂量为 3.28 mg/kg 时，小鼠没有表现出总胆固醇降低，然而剂量为 16.4 mg/kg 时显示显著降低了总胆固醇血浆水平约 10%，并表现出优异的生物利用度[1]。
Name	PCSK9-IN-13
CAS	2244129-23-3
Formula	C30H33N5O2
Molar Mass	495.62
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Benny J. Evison, et al. A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.Bioorganic & Medicinal Chemistry

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