Thiamet G | O-GlcNAcase antagonist

CAS:
1009816-48-1
Catalog Number:
10-2824
Activity:
O-GlcNAcase alpha 1 antagonist
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:
248.30
Molecular Formula:
C9H16N2O4S
Solubility:
Soluble in DMSO (up to 10 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
5 mg$70.00
25 mg$260.00

Thiamet G (1009816-48-1) is a 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 Thiamet G prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice.3 Elevates soluble tau species and reduces tauopathy in mouse models.Active in vivo and blood brain barrier permeable.

References/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
4) Hastings et al. (2017) Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice; Mol. Neurodegener., 12 39

CAS:
1009816-48-1
Catalog Number:
10-2824
Activity:
O-GlcNAcase alpha 1 antagonist
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:
248.30
Molecular Formula:
C9H16N2O4S
Solubility:
Soluble in DMSO (up to 10 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee