Cat. No. Name Size Price Add Cart
KI1142LY28867215 mg$272
LY288672110 mg$512
LY288672150 mg$1552
LY2886721200 mg$3952

Chemical Characteristic

Product NameLY2886721
CAS No.1262036-50-9
Molecular Weight 390.41
FormulaC18H16F2N4O2S
Smilesc1(ccc(cn1)F)C(=O)Nc1cc(c(cc1)F)C12N=C(SC[C@@H]1COC2)N
Chemical Structure

Biological activities

LY2886721 is a new BACE1 inhibitor. LY2886721 inhibits recombinant hBACE1 with an IC50 of 20.3 nM. In cellular assays, LY2886721 inhibits Aβ in HEK293Swe and PDAPP neuronal culture with IC50 of 18.7 and 10.7 nM, respectively.[1] LY2886721 dose-dependently decreases CSF sAPPβ and increases CSF sAPPα.[2] Oral administration of LY2886721 to PDAPP mice produces dose-dependent reductions in brain Aβ, C99 and sAPPβ. Brain Aβ levels are decreased by 20% -65% relative to vehicle-treated groups 3 hours after a 3-30 mg/kg dose of LY2886721. [1] LY2886721 dose-dependently lowers Aβs in animals. In the MAD study, LY2886721 dose-dependently lowers plasma and CSF Aβs. [2]

References

[1] May P, et al. Preclinical characterization of LY2886721: A BACE1 inhibitor in clinical development for early Alzheimer's disease. Alzheimer's & Dementia, 2012, 8(4), Supplement: 704-705.
[2] Martenyi F, et al. BACE inhibitor LY2886721 safety and central and peripheral PK and PD in healthy subjects (HSs). Alzheimer's & Dementia, 2012, 8(4), Supplement: 583-584.

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