For research use only. Not for therapeutic Use.
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].
PCSK9-IN-10 (compound 3s) (0, 2.5, 5, 12.5, 25 µM; 24 h) significantly decreases the PCSK9 protein expression and increases the expression of LDL receptor (LDLR) in a dose dependent manner[1].
PCSK9-IN-10 (30 mg/kg; p.o.; once a day for 8 weeks) reduces total cholesterol (TC) and atherosclerotic plaque size in ApoE KO mice[1].
Catalog Number | I042276 |
CAS Number | 368434-98-4 |
Synonyms | 8-(2-methoxyethylamino)-7-[(3-methoxyphenyl)methyl]-1,3-dimethylpurine-2,6-dione |
Molecular Formula | C18H23N5O4 |
Purity | ≥95% |
InChI | InChI=1S/C18H23N5O4/c1-21-15-14(16(24)22(2)18(21)25)23(17(20-15)19-8-9-26-3)11-12-6-5-7-13(10-12)27-4/h5-7,10H,8-9,11H2,1-4H3,(H,19,20) |
InChIKey | YUNMPASCLGGSKE-UHFFFAOYSA-N |
SMILES | CN1C2=C(C(=O)N(C1=O)C)N(C(=N2)NCCOC)CC3=CC(=CC=C3)OC |
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. |