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Chemical Structure| 1262036-50-9 Chemical Structure| 1262036-50-9

Structure of LY2886721
CAS No.: 1262036-50-9

Chemical Structure| 1262036-50-9

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LY2886721 is an effective, selective, orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM against recombinant human BACE1. LY2886721 exhibits selectivity for BACE1 over tissue proteases D, gastric protease, and renin, but lacks selectivity for BACE2 (IC50 of 10.2 nM). LY2886721 crosses the blood-brain barrier and can be used in Alzheimer's disease research.

Synonyms: β-Secretase

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Product Details of LY2886721

CAS No. :1262036-50-9
Formula : C18H16F2N4O2S
M.W : 390.41
SMILES Code : O=C(NC1=CC=C(F)C([C@@]23N=C(N)SC[C@]2([H])COC3)=C1)C4=NC=C(F)C=C4
Synonyms :
β-Secretase
MDL No. :MFCD22124078

Safety of LY2886721

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
hippocampal slices 3 µM 2 hours LY2886721 reduced mouse Aβ1-42 levels and reversed the sevo-induced upregulation of Aβ1-42. PMC9223703
human platelets 10 μM 30 minutes To investigate the effect of LY2886721 on the release of Aβ1-42 and Aβ1-40 from human platelets, the results showed that LY2886721 had no effect on the release of these peptides. PMC7614566
Rat cortical neurons 0.04 μM 4 days LY2886721 treatment at 0.04 μM showed a trend towards decreased secretion of Aβ40 (39%), but did not significantly affect synaptic transmission. PMC7251689
Rat cortical neurons 0.3 μM 4 days LY2886721 treatment at 0.3 μM significantly decreased Aβ40 secretion (53%), but did not significantly affect synaptic transmission. PMC7251689
Rat cortical neurons 3 μM 4 days LY2886721 treatment at 3 μM significantly decreased Aβ40 (57%) and Aβ42 (57%) secretion and significantly reduced synaptic transmission (39%). PMC7251689
PS1-S170F iPSC-derived neurons 5 μM 5 days To investigate the effects of LY2886721 on Aβ42 and p-Tau levels, results showed significant reduction in Aβ42 and p-Tau levels PMC7162796

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats McGill-R-Thy1-APP transgenic rats Intracerebroventricular injection 0.2 nmol Five injections over three days LY2886721 reversed the LTP deficit in 4.5-month-old TG rats, but the effect was transient, lasting less than a week. PMC4293804

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01367262 Healthy Volunteers PHASE1 COMPLETED 2025-07-11 For additional information reg... More >>arding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Madison, Wisconsin, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.81mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL

References

 

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