Thiamet GDiscontinued
- Product Name
- Thiamet GDiscontinued
- CAS No.
- 1009816-48-1
- Chemical Name
- Thiamet GDiscontinued
- Synonyms
- CS-1700;Thiamet G;Thiamet H;Thiamet G - Bio-X ?;Thiamet G (Thiamet-G);Thiamet G0nDiscontinued;Thiamet GDiscontinued;Thiamet G, 10 mM in DMSO;Thiamet G_x000b_Discontinued;Thiamet G, O-GlcNAcase inhibitor
- CBNumber
- CB52485666
- Molecular Formula
- C9H16N2O4S
- Formula Weight
- 248.3
- MOL File
- 1009816-48-1.mol
Thiamet GDiscontinued Property
- 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
- Water Solubility
- H2O: ≥5mg/mL atwarmed to 60°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.
- InChI
- InChI=1S/C9H16N2O4S/c1-2-10-9-11-5-7(14)6(13)4(3-12)15-8(5)16-9/h4-8,12-14H,2-3H2,1H3,(H,10,11)/t4-,5-,6-,7-,8-/m1/s1
- InChIKey
- PPAIMZHKIXDJRN-UKPHHSARSA-N
- SMILES
- S1[C@@]2([H])O[C@H](CO)[C@@H](O)[C@H](O)[C@@]2([H])N=C1NCC
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- SML0244
- Product name
- Thiamet G
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $131
- Updated
- 2025/07/31
- Product number
- SML0244
- Product name
- Thiamet G
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $493.05
- Updated
- 2025/07/31
- Product number
- 13237
- Product name
- Thiamet G
- Purity
- ≥97%
- Packaging
- 1mg
- Price
- $40
- Updated
- 2024/03/01
- Product number
- 13237
- Product name
- Thiamet G
- Purity
- ≥97%
- Packaging
- 5mg
- Price
- $89
- Updated
- 2024/03/01
- Product number
- 13237
- Product name
- Thiamet G
- Purity
- ≥97%
- Packaging
- 10mg
- Price
- $133
- Updated
- 2024/03/01
Thiamet GDiscontinued Chemical Properties,Usage,Production
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
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.
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
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.
in vivo
Thiamet G (500 mg/kg/d) increases global and tau O-GlcNAc and reduces neurodegeneration. Thiamet G-treated group has 1.4-fold more motor neurons and hinders tau-driven neurodegeneration within this transgenic model. Thiamet G treatment therefore has no detectable effect on mice lacking the P301L transgene, indicating that prevention of neurodegeneration and weight loss is mediated by Thiamet G treatment only in the context of the P301L transgene. In Thiamet G-treated mice, the O-GlcNAc increases in the brain and spinal cord tissues[1].
Thiamet G (20 mg/kg, i.p.) increases O-GlcNAc levels in brain, liver, and knee of the C57BL/6 mice in a dose-dependent manner[2].
storage
Store at -20°C
References
[1] SCOTT A YUZWA. A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo[J]. Nature chemical biology, 2008, 4 8: 483-490. DOI:10.1038/nchembio.96
[2] SCOTT A YUZWA. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation[J]. Nature chemical biology, 2012, 8 4: 393-399. DOI:10.1038/nchembio.797
[3] SCOTT A YUZWA. Pharmacological inhibition of O-GlcNAcase (OGA) prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice.[J]. Molecular Neurodegeneration, 2014, 9: 42. DOI:10.1186/1750-1326-9-42
[4] NICHOLAS B HASTINGS. Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice.[J]. ACS Combinatorial Science, 2017: 39. DOI:10.1186/s13024-017-0181-0
Thiamet GDiscontinued Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Thiamet GDiscontinued manufacturers
- Product
- Thiamet GDiscontinued 1009816-48-1
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 200kg
- Release date
- 2020-03-04
- Product
- Thiamet G 1009816-48-1
- Price
- US $9.80/KG
- Min. Order
- 1KG
- Purity
- >98%HPLC
- Supply Ability
- 20 tons
- Release date
- 2020-02-06