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Lp-PLA2-IN-3

CAS No. 2196245-16-4

Lp-PLA2-IN-3( —— )

Catalog No. M32996 CAS No. 2196245-16-4

Lp-PLA2-IN-3 is a potent, orally bioactive lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, effectively inhibiting recombinant human [Lp-PLA2] with an IC50 value of 14 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Lp-PLA2-IN-3
  • Note
    Research use only, not for human use.
  • Brief Description
    Lp-PLA2-IN-3 is a potent, orally bioactive lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, effectively inhibiting recombinant human [Lp-PLA2] with an IC50 value of 14 nM.
  • Description
    Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).
  • In Vitro
    ——
  • In Vivo
    Lp-PLA2-IN-3 (3 mg/kg; p.o.) treatment shows the Cmax, AUC0-24h, t1/2 and F were 0.27 μg/mL, 3.4 μg h/mL, 7.7 hours and 35.5%, respectively.Lp-PLA2-IN-3 (1 mg/kg; i.v.) treatment shows the CL, Vss, and t1/2 were 3.1mL/min/kg, 0.3 L/kg, 4 hours, respectively.Animal Model:Male Sprague?Dawley (SD) rats (180-220 g)Dosage:3 mg/kg Administration:p.o. (Pharmacokinetic Analysis)Result:The Cmax, AUC0-24h, t1/2 and F were 0.27 μg/mL, 6.2 μg h/mL, 7.7 hours and 35.5%, respectively.
  • Synonyms
    ——
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    Phospholipase
  • Recptor
    Phospholipase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2196245-16-4
  • Formula Weight
    467.85
  • Molecular Formula
    C20H13ClF3N3O3S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 250 mg/mL (534.36 mM )
  • SMILES
    Nc1ccc(cc1)S(=O)(=O)Nc1ccc(Oc2ccc(Cl)c(c2)C(F)(F)F)c(c1)C#N
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Liu Q, et al. Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2. J Med Chem. 2017 Dec 28;60(24):10231-10244.?
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