A potent and selective inhibitor of O-GlcNAcase (Ki = 21 nM); increases cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day); is orally bioavailable and effectively cross the blood brain barrier

Thiamet G – 5 mg

Brand:
Cayman
CAS:
1009816-48-1
Storage:
-20
UN-No:
Non-Hazardous - /

Hyperphosphorylation of the tau protein leads to its aggregation and formation of neurofibrillary tangles, a hallmark of Alzheimer’s disease and other tauopathic, neurodegenerative disorders. Tau is also dynamically modified by the addition and cleavage of O-linked β-N-acetylglucosamine (O-GlcNAc) moieties, which is mediated in part by O-GlcNAcase. Levels of O-GlcNAcylated proteins from Alzheimer’s disease brain extracts are decreased as compared to that in controls, suggesting that impaired brain glucose metabolism may contribute to pathogenesis.{16842} Thiamet G is a potent and selective inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM.{16935} It increases cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day).{16935} Thiamet G is the first highly potent O-GlcNAcase inhibitor known to be orally bioavailable and effectively cross the blood brain barrier.{16935}  

 

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Description

A potent and selective inhibitor of O-GlcNAcase (Ki = 21 nM); increases cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day); is orally bioavailable and effectively cross the blood brain barrier

Formal name: 2-(ethylamino)-3aR,6S,7R,7aR-tetrahydro-5R-(hydroxymethyl)-5H-pyrano[3,2-d]thiazole-6,7-diol

Synonyms: 

Molecular weight: 248.3

CAS: 1009816-48-1

Purity: ≥97%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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