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Submit ReviewOrg 25543 hydrochloride is a potent and selective glycine transporter type 2 (GlyT2) inhibitor (IC50 = 16 nM for hGlyT2). Displays no activity at GlyT1 or 56 other common biological targets (≥ 100 μM), in a glycine uptake assay in CHO cells. Ameliorates mechanical allodynia after partial sciatic nerve ligation injury in mice.
Org 25543 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 448.98 |
Formula | C24H32lN2O4.HCl |
Storage | Desiccate at RT |
Purity | ≥99% (HPLC) |
CAS Number | 495076-64-7 |
PubChem ID | 10095215 |
InChI Key | NIPQJILJYQVZJR-UHFFFAOYSA-N |
Smiles | O=C(NCC2(N(C)C)CCCC2)C1=CC(OC)=C(OCC3=CC=CC=C3)C(OC)=C1.Cl |
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 | |
---|---|---|---|
Solubility | |||
water | 8.98 | 20 | |
DMSO | 44.9 | 100 |
The following data is based on the product molecular weight 448.98. 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 | 2.23 mL | 11.14 mL | 22.27 mL |
5 mM | 0.45 mL | 2.23 mL | 4.45 mL |
10 mM | 0.22 mL | 1.11 mL | 2.23 mL |
50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
References are publications that support the biological activity of the product.
Caulfield et al (2001) The first potent and selective inhibitors of the glycine transporter type 2. J.Med.Chem. 44 2679 PMID: 11495577
Morita et al (2008) Spinal antiallodynia action of glycine transporter inhibitors in neuropathic pain models in mice. J.Pharmacol.Exp.Ther. 326 633 PMID: 18448867
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