LY2886721

Catalog No.S2156

LY2886721 Chemical Structure

Molecular Weight(MW): 390.41

LY2886721 is a BACE inhibitor used for the treatment of Alzheimer's Disease. Phase 1/2.

Size Price Stock Quantity  
In DMSO USD 270 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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  • Cell Discov, 2015, 1:15021.. LY2886721 purchased from Selleck.

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Choose Selective BACE Inhibitors

Biological Activity

Description LY2886721 is a BACE inhibitor used for the treatment of Alzheimer's Disease. Phase 1/2.
Targets
BACE2 [4]
(Cell-free assay)
BACE1 [4]
(Cell-free assay)
10.2 nM 20.3 nM
In vitro

LY2886721 is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the clinical progression of AD. [1] LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid[2]. LY2886721 inhibits recombinant hBACE1 with an IC50 of 20.3 nM. In cellular assays, LY2886721 inhibits Abeta with an IC50 of 18.7 nM and 10.7 nM, HEK293Swe and PDAPP neuronal culture, respectively[3]. LY2886721 has high selectivity against key off-target proteases, which efficiently translates in vitro activity into robust in vivo amyloid β lowering in nonclinical animal models. Assessment of LY2886721 activity against hBACE2 demonstrates an IC50 of 10.2 nM. Assessment of LY2886721 activity against cathepsin D, pepsin, renin, or other important aspartyl proteases shows essentially no inhibition (IC50 >100,000 nM), suggesting that activity against these common aspartyl proteases is unlikely to be significant[4].

In vivo Oral administration of LY2886721 to PDAPP mice produces dose-dependent reductions in brain Abeta, C99 and sAPPbeta. Brain Abeta levels are decreased ∼20%-65% relative to vehicle-treated groups three hours after a 3-30 mg/kg dose of LY2886721. Brain C99 and sAPPb levels also are reduced in a dose-dependent manner consistent with BACE1 inhibition in vivo. The pharmacodynamic responses to LY2886721 persists out to 9 hours post dose in brains of PDAPP mice. Pharmacodynamic studies in beagle dog reveal robust and sustained reductions in plasma Abeta following 1 mg/kg LY2886721 dosing. Central effects of BACE1 inhibition in dog are manifested by a 50% reduction in CSF Abeta at 9 hours after a 0.5 mg/kg dose of LY2886721[3]. The geometric mean terminal elimination t1/2 is determined to be 17.2 h (range 8.19-36.3 h). The geometric mean apparent oral clearance is 34.8 L/h (38% CV) and the apparent volume of distribution during the terminal phase was 863 L (56% CV) across dose levels. LY2886721 is freely permeable across the blood-brain barrier[4].

Protocol

Cell Research:

[4]

+ Expand
  • Cell lines: HEK293 cells
  • Concentrations: --
  • Incubation Time: Overnight exposure
  • Method:

    A human embryonic kidney cell line (HEK293) stably expressing APP751cDNA containing a Swedish mutation (HEK293Swe) was exposed to increasing concentrations of LY2886721 and the amount of amyloid β1–40 (Aβ1-40) and Aβ1-42 measured in the media as an index of BACE1 inhibition. Compound cytotoxicity was assessed using a CellTiter96 Aqueous Non-Radioactive Cell Proliferation assay


    (Only for Reference)
Animal Research:

[4]

+ Expand
  • Animal Models: young PDAPP transgenic mice
  • Formulation: 7% Pharmasolve
  • Dosages: 1.5 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 9 mg/mL (23.05 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 390.41
Formula

C18H16F2N4O2S

CAS No. 1262036-50-9
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01807026 Completed Alzheimer Disease|Healthy Volunteers Eli Lilly and Company March 2013 Phase 1
NCT01775904 Completed Healthy Volunteers Eli Lilly and Company February 2013 Phase 1
NCT01561430 Terminated Alzheimers Disease Eli Lilly and Company March 2012 Phase 1|Phase 2
NCT01534273 Completed Healthy Volunteers Eli Lilly and Company February 2012 Phase 1
NCT01367262 Completed Healthy Subjects Eli Lilly and Company June 2011 Phase 1
NCT01227252 Completed Alzheimers Disease Eli Lilly and Company December 2010 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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BACE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID