LY2886721 hydrochloride
Based on 2 publication(s) in Google Scholar
LY2886721 hydrochloride 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 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
For research use only. We do not sell to patients.
- CAS No.: 1262036-49-6
- Formula: C18H17ClF2N4O2S
- Molecular Weight:426.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) LY2886721 hydrochloride
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Biological Activity
IC50: 20.3 nM (Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)); 10.2 nM (BACE2)[1]
Overnight exposure of HEK293Swe cells to increasing concentrations of LY2886721 hydrochloride 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 hydrochloride 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1262036-49-6
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Molecular Weight 426.87
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Formula C18H17ClF2N4O2S
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SMILES
FC1=CN=C(C=C1)C(NC2=CC=C(C([C@@]34[C@]([H])(CSC(N)=N4)COC3)=C2)F)=O.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Rep
Depletion of the AD Risk Gene SORL1 Selectively Impairs Neuronal Endosomal Traffic Independent of Amyloidogenic APP Processing. [Abstract]2020 Jun 2;31(9):107719. PMID: 32492427 -
FASEB J
2021 May;35(5):e21445. PMID: 33774866
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY2886721 hydrochloride Related Classifications
HY-13240A Related Classifications
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