1. Neuronal Signaling
    Stem Cell/Wnt
  2. γ-secretase
  3. ELN 318463

ELN 318463 

Cat. No.: HY-50882
Handling Instructions

ELN 318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN 318463 is 51-fold more selective for PS1.

For research use only. We do not sell to patients.

ELN 318463 Chemical Structure

ELN 318463 Chemical Structure

CAS No. : 851600-86-7

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Description

ELN 318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN 318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN 318463 is 51-fold more selective for PS1[1][2].

IC50 & Target

EC50: 12 nM (PS1 γ-secretase), 656 nM (PS2 γ-secretase)[1]

In Vitro

ELN 318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate[2].

In Vivo

ELN318463 (30 mg/kg or 100 mg/kg; orally) leads acute reduction of brain Aβ in in the PDAPP transgene model of Alzheimer's disease (AD) as well as in wild-type FVB strain mice[2].

Animal Model: Female, two- to three-month old, FVB/N mice and PDAPP transgene model of Alzheimer's disease (AD)[2]
Dosage: 30 mg/kg or 100 mg/kg
Administration: Orally
Result: Brain levels at 30 mg/kg were 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains.
Molecular Weight

471.80

Formula

C₁₉H₂₀BrClN₂O₃S

CAS No.

851600-86-7

SMILES

O=S(N(CC1=CC=C(Br)C=C1)[[email protected]]2C(NCCCC2)=O)(C(C=C3)=CC=C3Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ELN 318463ELN318463ELN-318463γ-secretaseGamma secretaseamyloidprecursorproteinAPPpresenilinPS1PS2NotchAlzheimerdiseaseInhibitorinhibitorinhibit

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ELN 318463
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HY-50882
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