1. Neuronal Signaling
  2. Beta-secretase
  3. Elenbecestat

Elenbecestat (Synonyms: E2609)

Cat. No.: HY-109055 Purity: 99.77%
Handling Instructions

Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.

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

Elenbecestat Chemical Structure

Elenbecestat Chemical Structure

CAS No. : 1388651-30-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 284 In-stock
Estimated Time of Arrival: December 31
5 mg USD 295 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
25 mg USD 965 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1640 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research[1][2].

IC50 & Target

BACE-1[1]

In Vitro

Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay[2].
Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents[2].

In Vivo

Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates[2].
Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing[1].

Animal Model: Cynomolgus monkeys (Pharmacokinetic analysis)[2]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 30 mg/kg
Administration: Oral administration
Result: Potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF.
Clinical Trial
Molecular Weight

437.44

Formula

C₁₉H₁₈F₃N₅O₂S

CAS No.

1388651-30-6

SMILES

FC1=CC=C(NC(C2=NC=C(C(F)F)N=C2)=O)C=C1[[email protected]@]3(N=C(N)SC4)[[email protected]@]4([H])[[email protected]@H](C)OC3

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 : ≥ 250 mg/mL (571.51 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2860 mL 11.4301 mL 22.8603 mL
5 mM 0.4572 mL 2.2860 mL 4.5721 mL
10 mM 0.2286 mL 1.1430 mL 2.2860 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 (4.75 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

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

ElenbecestatE2609E 2609E-2609Beta-secretaseBACEβ-SecretaseBACE-1Alzheimer's diseaseADInhibitorinhibitorinhibit

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Product Name:
Elenbecestat
Cat. No.:
HY-109055
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