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PF-06751979

Chemical Structure : PF-06751979

CAS No.: 1818339-66-0

PF-06751979 (PF06751979)

Catalog No.: PC-63290Not For Human Use, Lab Use Only.

PF-06751979 is a potent, selective, brain penetrant BACE1 inhibitor with binding IC50 of 7.3, 27-fold selectivity over BACE2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-06751979 is a potent, selective, brain penetrant BACE1 inhibitor with binding IC50 of 7.3, 27-fold selectivity over BACE2.
PF-06751979 shows BACE1 inhibition and sAPPβ production in whole-cell assay with IC50 of 5.1 and 5 nM.
PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases including BACE2; demonstrates potent and dose-dependent Aβ lowering in human CSF with lacking hypopigmentation compared with AZD3239.

Physicochemical Properties

M.Wt 455.499
Formula C18H19F2N5O3S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-((4aR,6S,8aR)-2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl)thiazol-4-yl)-5-(difluoromethoxy)picolinamide

References

1. O'Neill BT, et al. J Med Chem. 2018 Apr 3. doi: 10.1021/acs.jmedchem.8b00246.

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