Other grades of this product :
| Thiamet GDiscontinued Basic information |
| Product Name: | Thiamet GDiscontinued | | Synonyms: | Thiamet GDiscontinued;Thiamet G;1,2-Dideoxy-2'-ethylamino-a-D-glucopyranoso-[2,1-d]-2'-thiazoline;2-(ethylaMino)-5-(hydroxyMethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-dio;5H-Pyrano[3,2-d]thiazole-6,7-diol, 2-(ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-, (3aR,5R,6S,7R,7aR)-;(3aR,5R,6S,7R,7aR)-2-(ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-5H-Pyrano[3,2-d]thiazole-6,7-diol;(3aR,5R,6S,7R,7aR)-2-(Ethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol;Thiamet G0nDiscontinued | | CAS: | 1009816-48-1 | | MF: | C9H16N2O4S | | MW: | 248.3 | | EINECS: | | Product Categories: | Carbohydrates & Derivatives;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;API;Intermediates | | Mol File: | 1009816-48-1.mol |
| Thiamet GDiscontinued Chemical Properties |
| Boiling point | 483.2±55.0 °C(Predicted) | | density | 1.74±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | H2O: ≥5mg/mL at warmed to 60°C | | form | powder | | pka | 13.17±0.70(Predicted) | | color | white to beige | | optical activity | [α]/D -21 to -26°, c = 0.3 in methanol | | 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. | | InChIKey | PPAIMZHKIXDJRN-UKPHHSARSA-N |
| Thiamet GDiscontinued Usage And Synthesis |
| Description | 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.4?Active?in vivo?and blood brain barrier permeable. | | Uses | As a potent O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo, The authors anticipate that Thiamet-G will find wide use in probing the functional role of O-GlcNAc in vertebrate brain, and it may also offer a route to blocking pathological
| | Uses | A potent O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. The authors anticipate that Thiamet-G will find wide use in probing the functional role of O-GlcNAc in vertebrate brain, and it may also offer a route to blocking pathological hyperphosphorylation of tau in AD. Anti-Alzheimer''s agent. | | Biochem/physiol Actions | Thiamet G is a potent inhibitor of the enzyme O-GlcNAcase (Ki = 21 nM). The compound is orally bioavailable and crosses the blood brain barrier. Thiamet G leads to an increase in O-GlcNAc-modified proteins in cell-based and in vivo assay systems, and reduces levels of phosphorylated Tau protein in rat cortex and hippocampus. | | References | 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 |
| Thiamet GDiscontinued Preparation Products And Raw materials |
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