E2012

E2012

CAT N°: 29710
Price:

From 146.00 124.10

E2012 is a modulator of ?-secretase.{48834} It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-? (A?) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by ?-secretase, when used at a concentration of 1 µM in luciferase assays.{48835} E2012 also inhibits the activity of the cholesterol synthesis enzyme 3?-hydroxysterol ?24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).{48836} It reduces A? (1-42) (A?42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.{48837} E2012 (100 mg/kg) also decreases A?42 levels in guinea pig brain and cerebral spinal fluid (CSF).{48837}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methylene]-2-piperidinone
  • Correlated keywords
    • 1058171-26-8 E 2012 hydroxy sterol ? 24 DHCR 24 Hep G2 A? 42
  • Product Overview:
    E2012 is a modulator of ?-secretase.{48834} It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-? (A?) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by ?-secretase, when used at a concentration of 1 µM in luciferase assays.{48835} E2012 also inhibits the activity of the cholesterol synthesis enzyme 3?-hydroxysterol ?24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).{48836} It reduces A? (1-42) (A?42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.{48837} E2012 (100 mg/kg) also decreases A?42 levels in guinea pig brain and cerebral spinal fluid (CSF).{48837}

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