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Submit ReviewTP-040 is a potent and selective O-GlcNAcase (OGA) inhibitor (IC50 = 46 nM). It increases the level of O-GlcNAcylated protein in human neuroblastoma SH-SY5Y cells (EC50 = 450 nM). It is suitable for in vivo studies and exhibits brain permeability.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the TP-040 probe summary on the SGC website.
分子量 | 286.38 |
公式 | C15H22N6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2757254-99-0 |
PubChem ID | 162640825 |
InChI Key | PWKAYICUBVNJAZ-UHFFFAOYSA-N |
Smiles | CN1C=NC(CNC2=NC=CC(N3CCC(CC3)C)=N2)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 28.64 | 100 | |
DMSO | 28.64 | 100 |
以下数据基于产品分子量 286.38。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.49 mL | 17.46 mL | 34.92 mL |
5 mM | 0.7 mL | 3.49 mL | 6.98 mL |
10 mM | 0.35 mL | 1.75 mL | 3.49 mL |
50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
参考文献是支持产品生物活性的出版物。
Tawada et al (2021) Discovery of a novel and brain-penetrant O-GlcNAcase inhibitor via virtual screening, structure-based analysis, and rational lead optimization. J.Med.Chem. 64 1103 PMID: 33404239
If you know of a relevant reference for TP-040, please let us know.
关键词: TP-040, TP-040 supplier, potent, selective, O-GlcNAcase, inhibitor, inhibits, OGA, increase, O-GlcNAcylation, brain, permeable, Other, Hydrolases, 7771, Tocris Bioscience
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