1. Neuronal Signaling
    Stem Cell/Wnt
  2. γ-secretase
  3. ELN318463

ELN318463 

Cat. No.: HY-50882 Purity: 99.33%
Handling Instructions

ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1.

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

ELN318463 Chemical Structure

ELN318463 Chemical Structure

CAS No. : 851600-86-7

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5 mg USD 800 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1300 In-stock
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50 mg USD 3500 In-stock
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100 mg USD 4900 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 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

ELN318463 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (264.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1195 mL 10.5977 mL 21.1954 mL
5 mM 0.4239 mL 2.1195 mL 4.2391 mL
10 mM 0.2120 mL 1.0598 mL 2.1195 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ELN318463ELN 318463ELN-318463γ-secretaseGamma secretaseamyloidprecursorproteinAPPpresenilinPS1PS2NotchAlzheimerdiseaseInhibitorinhibitorinhibit

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Product Name:
ELN318463
Cat. No.:
HY-50882
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