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Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 < 4). Active in vivo.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||1.84||5 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 367.36. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.72 mL||13.61 mL||27.22 mL|
|5 mM||0.54 mL||2.72 mL||5.44 mL|
|10 mM||0.27 mL||1.36 mL||2.72 mL|
|50 mM||0.05 mL||0.27 mL||0.54 mL|
References are publications that support the biological activity of the product.
Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID: 23194655
Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID: 11454468
Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID: 12963052
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Keywords: Org 24598, Org 24598 supplier, Org24598, glial, glycine, transporters, glyt1, inhibitors, inhibits, Glycine, Transporters, 4447, Tocris Bioscience
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Literature in this Area
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Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.