A γ-secretase modulator; selectively inhibits AICD cleavage to Aβ over Notch cleavage to NICD at 1 µM in luciferase assays; inhibits DHCR24 activity in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM

E2012 – 50 mg

Brand:
Cayman
CAS:
870843-42-8
Storage:
-20
UN-No:
Non-Hazardous - /

E2012 is a modulator of γ-secretase.{48834} It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.{48835} E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).{48836} It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.{48837} E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).{48837}  

 

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SKU: 29710 - 50 mg Category:

Description

A γ-secretase modulator; selectively inhibits AICD cleavage to Aβ over Notch cleavage to NICD at 1 µM in luciferase assays; inhibits DHCR24 activity in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively); reduces Aβ42 production in primary rat embryonic cerebral cortex neurons (IC50 = 220 nM); decreases Aβ42 levels in guinea pig brain and CSF at 100 mg/kg

Formal name: (3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]methylene]-2-piperidinone

Synonyms: 

Molecular weight: 419.5

CAS: 870843-42-8

Purity: ≥98%

Formulation: A solid

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