1. Neuronal Signaling
  2. Beta-secretase
  3. LY2886721

LY2886721 

Cat. No.: HY-13240 Purity: 99.92%
Handling Instructions

LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.

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

LY2886721 Chemical Structure

LY2886721 Chemical Structure

CAS No. : 1262036-50-9

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 468 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment[1].

IC50 & Target

IC50: 20.3 nM (Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)); 10.2 nM (BACE2)[1]

In Vitro

Overnight exposure of HEK293Swe cells to increasing concentrations of LY2886721 shows a concentration-dependent decrease in the amount of Aβ secreted into the condition medium. Consistent with a mechanism of BACE inhibition, the EC50s for inhibition of Aβ1-40 and Aβ1-42 are essentially identical, 18.5 and 19.7 nM, respectively[1].
Overnight exposure of PDAPP neuronal cultures to an increasing concentration of LY2886721 produces a concentration-dependent decrease in Aβ production. As observed in HEK293Swe cells, the EC50s for inhibition of Aβ1-40 and Aβ1-42 are comparable in PDAPP neuronal cultures at ∼10 nM[1].

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

In Vivo

LY2886721 (3-30 mg/kg; oral administration; PDAPP mice) treatment significantly reduces the hippocampal and cortical levels of Aβ1-x. LY2886721 treatment results in significant reduction of brain parenchymal levels of C99 and sAPPβ[1].

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

Animal Model: Female hemizygous APPV717F transgenic mice (PDAPP) (2-3 months old)[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Hippocampal and cortical levels of Aβ1-x were significantly reduced.
Clinical Trial
Molecular Weight

390.41

Formula

C₁₈H₁₆F₂N₄O₂S

CAS No.

1262036-50-9

SMILES

FC1=CN=C(C=C1)C(NC2=CC=C(C([[email protected]@]34[[email protected]]([H])(CSC(N)=N4)COC3)=C2)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 20 mg/mL (51.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5614 mL 12.8070 mL 25.6141 mL
5 mM 0.5123 mL 2.5614 mL 5.1228 mL
10 mM 0.2561 mL 1.2807 mL 2.5614 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2 mg/mL (5.12 mM); Clear solution

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

Purity: 99.92%

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Keywords:

LY2886721LY 2886721LY-2886721Beta-secretaseBACEβ-SecretaseAlzheimer'sdiseaseBACE1BACE2BBBC99sAPPβInhibitorinhibitorinhibit

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LY2886721
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HY-13240
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