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    LY2886721
    LY2886721

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1312
    CAS #: 1262036-50-9 Purity ≥98%

    Description: LY2886721 (LY 2886721; LY-2886721) is a novel, potent and selective BACE (β-secretase) inhibitor with the potential for the treatment of AD-Alzheimer's Disease. BACE1 is a key protease controlling the formation of amyloid β, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease (AD). LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans. 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. 

    References: J Alzheimers Dis. 2011;24 Suppl 2:43-52; J Neurosci. 2015 Jan 21;35(3):1199-210. 

    Related CAS#: 262036-49-6 (HCl )

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    Molecular Weight (MW)390.41
    FormulaC18H16F2N4O2S 
    CAS No.1262036-50-9  (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 9 mg/mL (23.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide
    InChi Key: NIDRNVHMMDAAIK-YPMLDQLKSA-N
    InChi Code: InChI=1S/C18H16F2N4O2S/c19-11-1-4-15(22-6-11)16(25)23-12-2-3-14(20)13(5-12)18-9-26-7-10(18)8-27-17(21)24-18/h1-6,10H,7-9H2,(H2,21,24)(H,23,25)/t10-,18-/m0/s1
    SMILES Code: O=C(NC1=CC=C(F)C([[email protected]@]23N=C(N)SC[[email protected]]2([H])COC3)=C1)C4=NC=C(F)C=C4
    SynonymsLY2886721; LY-2886721; LY 2886721


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    In Vitro

    In vitro activity: 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. LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid.


    Cell Assay: treatment of LY2886721 leads to the inhibition of Aβ in HEK293Swe with IC50 of 18.7nM and PDAPP neuronal culture with IC50 10.7 nM1. LY2886721 decreases CSF sAPPβ and increases CSF sAPPα in a dose- dependent manner 2. 

    In VivoAt all 3 doses, LY2886721 significantly reduced hippocampal and cortical levels of Aβ1-x. In addition, LY2886721 significantly lowered brain parenchymal levels of C99 and sAPPβ. Although cortical levels of C99 were reduced significantly by LY2886721 at the doses of 10 and 30 mg/kg, the effect of LY2886721 at the dose of 3 mg/kg failed to reach statistical significance. On the other hand, the sAPPβ levels were significantly decreased by LY2886721 at all 3 doses. 
    Animal modelPDAPP mice 
    Formulation & Dosage3-30 mg/kg  
    ReferencesJ Alzheimers Dis. 2011;24 Suppl 2:43-52; J Neurosci. 2015 Jan 21;35(3):1199-210. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    LY2886721

    Pharmacologic effects in vivo of oral administration of LY2886721. J Neurosci.2015 Jan 21;35(3):1199-210. 
     

    LY2886721

    Peripheral and central PD effects of LY2886721 in beagle dogs after a single 1.5 mg/kg dose. J Neurosci. 2015 Jan 21;35(3):1199-210. 
     

    LY2886721

    Plasma Aβ species by time course in humans after administration of a single dose of 5, 7, 10, 15, 25, 35, and 70 mg of LY2886721 in healthy subjects. J Neurosci. 2015 Jan 21;35(3):1199-210. 


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