Avagacestat

Avagacestat

CAT N°: 16711
Price:

From 66.00 56.10

?-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and ?-amyloid precursor protein (APP), within the transmembrane domain.{27051,25415} Avagacestat is a potent, orally bioavailable inhibitor of ?-secretase that more potently inhibits the cleavage of APP to A?40 than signaling through Notch (IC50s = 0.30 and 58 nM, respectively).{27425} It shows good pharmacokinetics in rats, dogs, and humans and passes the blood-brain barrier, reducing plasma, brain, and cerebrospinal fluid A?40 levels.{27425,27428} While suppressing the production of A?38, A?40, and A?42, ?-secretase inhibitors, including avagacestat, increase the level of APP ?-C-terminal fragment, both in vitro and in vivo, altering cell function.{27426} Avagacestat may impact Notch signaling in vivo, although it is generally considered a “Notch-sparing” ?-secretase inhibitor.{27427}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoro-pentanamide
  • Correlated keywords
    • biochemical inhibitor Alzheimer’s research neuroscience BMS708163 inhibit ?-secretase protease enzyme complex cleave single-pass transmembrane protein Notch receptor ?-amyloid precursor protein ?APP ?-APP domain orally bioavailable cleavage A?40 pharmacokinetic rat dog human blood-brain barrier BBB plasma brain cerebrospinal fluid CSF reduce level A?38 A?42 increase ?-C-terminal fragment ?CTF in vitro vivo cell function Notch-sparing BMS 708163-01
  • Product Overview:
    ?-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and ?-amyloid precursor protein (APP), within the transmembrane domain.{27051,25415} Avagacestat is a potent, orally bioavailable inhibitor of ?-secretase that more potently inhibits the cleavage of APP to A?40 than signaling through Notch (IC50s = 0.30 and 58 nM, respectively).{27425} It shows good pharmacokinetics in rats, dogs, and humans and passes the blood-brain barrier, reducing plasma, brain, and cerebrospinal fluid A?40 levels.{27425,27428} While suppressing the production of A?38, A?40, and A?42, ?-secretase inhibitors, including avagacestat, increase the level of APP ?-C-terminal fragment, both in vitro and in vivo, altering cell function.{27426} Avagacestat may impact Notch signaling in vivo, although it is generally considered a “Notch-sparing” ?-secretase inhibitor.{27427}

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