368434-98-4
368434-98-4 structure
- Name: PCSK9-IN-10
- Chemical Name: PCSK9-IN-10
- CAS Number: 368434-98-4
- Molecular Formula: C18H23N5O4
- Molecular Weight: 373.41
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Ser/Thr Protease
- Create Date: 2023-02-05 16:36:44
- Modify Date: 2024-01-10 20:54:57
-
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].
| Name | PCSK9-IN-10 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| In Vitro | 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: HepG2 cells Concentration: 0-1000 µM Incubation Time: 24 h Result: Showed low cytotoxicity to HepG2 cells. Western Blot Analysis[1] Cell Line: HepG2 cells Concentration: 0, 2.5, 5, 12.5, 25 µM Incubation Time: 24 h Result: Significantly decreased PCSK9 protein level in a dose dependent manner. |
| 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: Eight weeks old male ApoE KO mice[1] Dosage: 30 mg/kg Administration: P.o.; once a day for 8 weeks Result: Inhibited both hepatic and serum PCSK9 content obviously and reduced reduced atherosclerotic plaque size. |
| References |
| Molecular Formula | C18H23N5O4 |
|---|---|
| Molecular Weight | 373.41 |