| Bioactivity | PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia[1]. | |||||||||
| Invitro | PCSK9-IN-10 (compound 3s) (0, 2.5, 5, 12.5, 25 µM; 24 h) 以剂量依赖性方式显著降低 PCSK9 蛋白表达并增加 LDL 受体 (LDLR) 的表达[1]。 Cell Cytotoxicity Assay[1] Cell Line: | |||||||||
| In Vivo | PCSK9-IN-10 (30 mg/kg；口服；每天一次，持续 8 周) 降低 ApoE KO 小鼠的总胆固醇 (TC) 和动脉粥样硬化斑块大小[1]。 Animal Model: | |||||||||
| Name | PCSK9-IN-10 | |||||||||
| CAS | 368434-98-4 | |||||||||
| Formula | C18H23N5O4 | |||||||||
| Molar Mass | 373.41 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Qiao MQ, et al. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis. Eur J Med Chem. 2022 Dec 26;247:115047. |
PCSK9-IN-10
CAS: 368434-98-4 F: C18H23N5O4 W: 373.41
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expre
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