Thiamet GA potent and selective O-GlcNAcase inhibitor

Thiamet G (CAS 1009816-48-1)

Thiamet G | CAS 1009816-48-1 is rated 5.0 out of 5 by 2.
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Synonym: (3aR,5R,6S,7R,7aR)-2-(Ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-5H-pyrano[3,2-d]thiazole-6,7-diol
Application: A potent and selective O-GlcNAcase inhibitor
CAS Number: 1009816-48-1
Purity: ≥97%
Molecular Weight: 248.30
Molecular Formula: C9H16N2O4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Thiamet G is a potent, selective, and blood brain barrier permeable inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM. This compound has been shown to increase cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and block phosphorylation of tau protein both in cultured PC-12 cells and in rats. Research has shown that hyperphosphorylation of the tau protein can lead to its aggregation and subsequent 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.


References

1. Liu, F., et al. 2004. Proc. Natl. Acad. Sci. U.S.A. 101: 10804-10809. PMID: 15249677
2. Yuzwa, S.A., et al. 2008. Nat. Chem. Biol. 4: 483-490. PMID: 18587388

Physical State :
Solid
Solubility :
Soluble in water (3 mg/ml at 25.0° C), ethanol (~0.5 mg/ml), DMSO (~20 mg/ml), DMF (~20 mg/ml), and PBS(pH7.2) (~3 mg/ml).
Storage :
Store at -20° C
Boiling Point :
483.21° C at 760 mmHg (Predicted)
Density :
1.75 g/cm3 (Predicted)
Refractive Index :
n20D 1.73 (Predicted)
IC50 :
PC-12: EC5050 = 30 nM (rat)
Ki Data :
NCOAT: Ki= 21 nM (human)
pK Values :
pKa: 13.17 (Predicted), pKb: 6.43 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
24808478
MDL Number :
MFCD15144964
SMILES :
CCNC1=N[C@@H]2[C@H]([C@@H]([C@H](O[C@@H]2S1)CO)O)O

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Certificate of Analysis

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Rated 5 out of 5 by from good for OGlcNAcase inhibition I bought this inhibitor recently, it's good for OGlcNAcase inhibition.
Date published: 2016-10-28
Rated 5 out of 5 by from Yuzwa et al Yuzwa et al. (PubMed ID 18587388) showed that Thiamet G inhibited human O-GlcNAcase and reduced tau phosphorylation in PC-12 cells. -SCBT Publication Review
Date published: 2015-02-18
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