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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Thiamet G Exclusive

Cayman Chemical Item Number 13237

(CAS 1009816-48-1)

Thiamet G (CAS 1009816-48-1)

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Description

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.1 Thiamet G is a potent and selective inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM.2 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).2 Thiamet G is the first highly potent O-GlcNAcase inhibitor known to be orally bioavailable and effectively cross the blood brain barrier.2

1 Liu, F., Iqbal, K., Grundke-Iqbal, I., et al. O-GlnNAcylation regulates phosphorylation of tau: A mechanism involved in Alzheimer’s disease. Proc Natl Acad Sci USA 101(29) 10804-10809 (2004).

2 Yuzwa, S.A., Macauley, M.S., Heinonen, J.E., et al. A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. Nat Chem Biol 4(8) 483-490 (2008).

Formal Name 2-​(ethylamino)-​3aR,​6S,​7R,​7aR-​tetrahydro-​5R-​(hydroxymethyl)-​5H-​pyrano[3,​2-​d]thiazole-​6,​7-​diol
CAS Number 1009816-48-1
Molecular Formula C9H16N2O4S
Formula Weight 248.3
Formulation A crystalline solid
Purity ≥97%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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[H]​[C@@]​12[C@@]​(N=C(N(CC)​[H]​)​S2)​([H]​)​[C@@H]​(O)​[C@H]​(O)​[C@@H]​(CO)​O1

Background Reading

Liu, F., Iqbal, K., Grundke-Iqbal, I., et al. O-GlnNAcylation regulates phosphorylation of tau: A mechanism involved in Alzheimer’s disease. Proc Natl Acad Sci USA 101(29) 10804-10809 (2004).

Yuzwa, S.A., Macauley, M.S., Heinonen, J.E., et al. A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. Nat Chem Biol 4(8) 483-490 (2008).

Thiamet G is available in the following screening library:

Size Price Quantity Subtotal
500 µg $82.00 $0.00
1 mg $156.00 $0.00
5 mg $656.00 $0.00
10 mg $1,148.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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