PCSK9-IN-10

For research use only. Not for therapeutic Use.

  • CAT Number: I042276
  • CAS Number: 368434-98-4
  • Molecular Formula: C18H23N5O4
  • Molecular Weight: 373.41
  • Purity: ≥95%
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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.
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