Ceperognastat (LY3372689) | OGA inhibitor

Chemical Structure : LY3372689

CAS No.: 2241514-56-5

LY3372689 (Ceperognastat, LY-3372689)

Catalog No.: PC-72902Not For Human Use, Lab Use Only.

Ceperognastat (LY3372689) is a potent, selective and CNS-penetrant, orally bioavailable O-GlcNAcase (OGA) enzyme inhibitor with SPR KD of 133 pM (human OGA), IC50 of 2.4/1.8 nM for hOGA and mOGA respectively.

Packing	Price	Stock
5 mg	$238	In stock
10 mg	$378	In stock
25 mg	$598	In stock
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Biological Activity

Ceperognastat (LY3372689) is a potent, selective and CNS-penetrant, orally bioavailable O-GlcNAcase (OGA) enzyme inhibitor with SPR KD of 133 pM (human OGA), IC50 of 2.4/1.8 nM for hOGA and mOGA respectively.

Ceperognastat (LY3372689) binds OGA from different species with high affinity (1.8-2.4 nM) and displayed no difference in binding to brain homogenates from either AD or age-matched control brains.

Ceperognastat (LY3372689) demonstrates potent inhibition of purified human and mouse OGA and is highly selective against the functionally related lysosomal hexosaminidase enzymes HexA and HexB.

Ceperognastat (LY3372689) also shows no important in vitro binding activity across an industry standard selectivity panel of receptors, ion channels, transporters, and enzymes, and exhibited weak inhibition of the human ether-à-go-go (hERG) channel.

Ceperognastat (LY3372689) induces concentration-dependent increase in O-GlcNAc modified proteins in cellular assay with EC50 of 21.9 nM.

Ceperognastat (LY3372689) shows potential therapeutic approach to reduce the spread of tau pathology and thus slow the clinical progression of AD.

Physicochemical Properties

M.Wt	383.442
Formula	C16H22FN5O3S
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-(4-fluoro-5-(((2S,4S)-2-methyl-4-((5-methyl-1,2,4-oxadiazol-3-yl)methoxy)piperidin-1-yl)methyl)thiazol-2-yl)acetamide

References

1. Patent WO2018140299A1.
2. Kielbasa W, et al. Alzheimers Dement (N Y). 2024 Dec 26;10(4):e70020.

LY3372689 (Ceperognastat, LY-3372689)

Biological Activity

Physicochemical Properties

References

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