An inhibitor of BACE
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LY2886721

Item No. 21599

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[(4aS,7aS)-2-amino-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl]-5-fluoro-2-pyridinecarboxamide
CAS Number
1262036-50-9
Synonyms
  • β-Secretase
Molecular Formula
C18H16F2N4O2S
Formula Weight
390.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 9 mg/mlEthanol: <1 mg/mlWater: <1 mg/ml
λmax
279 nm
SMILES
FC1=CC=C(C(NC2=CC([C@@]34N=C(N)SC[C@]3([H])COC4)=C(F)C=C2)=O)N=C1
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
InChi Key
NIDRNVHMMDAAIK-YPMLDQLKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $223

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    10 mg

    $418

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    25 mg

    $717

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    Product Description

    LY2886721 selectively inhibits the β-site amyloid protein cleaving enzyme (BACE) (IC50 = 20 nM for recombinant hBACE1).1 BACE performs the first cleavage step in the Aβ cascade; thus, its inhibition by LY2886721 decreases production of all forms of the Aβ peptide.2 A Phase II clinical study for the use of LY2886721 in the treatment of Alzheimer’s disease was terminated early due to abnormal liver biochemistry values in several patients. The toxic effects did not appear to be due to BACE inhibition.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. May, P.C., Boggs, L.N., Brier, R., et al. Preclinical characterization of LY2886721: A BACE1 inhibitor in clinical development for early Alzheimer’s disease. J. Alzheim. Assoc. 8(4), 95 (2003).

    2. Vassar, R., Kovacs, D.M., Yan, R., et al. The beta-secretase enzyme BACE in health and Alzheimer’s disease: regulation, cell biology, function, and therapeutic potential. J. Neurosci. 29(41), 12787-12794 (2009).