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O-GlcNAcase alpha 1 antagonist CAS#: 1009816-48-1 Citations: 1) Yuzwa et al. (2008), A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo; Nat.Chem.Biol. 4 483 2) Yuzwa et al. (2012), Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation; Nat.Chem.Biol. 8 393 3) Yuzwa et al. (2014), Pharmacological inhibition of O-GlcNAcase (OGA) prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice; Mol.Neurodegener. 9 42

Product Code: ax132430 (5 mg)

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Product Specification

Function / pharmacology Potent, selective inhibitor of O-GlcNAcase (Ki = 21 nM for human O-GlcNAcase). Increases levels of O-GlcNAc-modified proteins in cellular assays and in vivo. Suppresses phosphorylation of tau protein in rat cortex and hippocampus.1 Stabilizes tau against aggregation and slows neurodegeneration.2 Prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice.3 Active in vivo and blood brain barrier permeable.
Chemical name (3aR,5R,6S,7R,7aR)-2-(Ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-5H-Pyrano[3,2-d]thiazole-6,7-diol
Molecular weight 248.3
Molecular formula C9H16N2O4S
Physical description Pale yellow solid
Solubility DMSO (10 mg/ml)
Size 5 mg
Stability Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.