PCSK9-IN-10

CAS No. 368434-98-4

PCSK9-IN-10( —— )

Catalog No. M36396 CAS No. 368434-98-4

PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 μM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 62 Get Quote
5MG 92 Get Quote
10MG 147 Get Quote
25MG 288 Get Quote
50MG 454 Get Quote
100MG 653 Get Quote
500MG 1368 Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    PCSK9-IN-10
  • Note
    Research use only, not for human use.
  • Brief Description
    PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 μM.
  • 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.
  • In Vitro
    Cell Cytotoxicity Assay Cell Line:HepG2 cells Concentration:0-1000 μM Incubation Time:24 h Result:Showed low cytotoxicity to HepG2 cells.Western Blot Analysis 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
    Animal Model:Eight weeks old male ApoE KO miceDosage: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.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Serine/threonin kinase
  • Recptor
    Serine/threonin kinase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    368434-98-4
  • Formula Weight
    373.41
  • Molecular Formula
    C18H23N5O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (669.51 mM; Ultrasonic )
  • SMILES
    COCCNc1nc2n(C)c(=O)n(C)c(=O)c2n1Cc1cccc(OC)c1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

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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