Biological Activity
Selective mGlu1 antagonist (Ki = 13 nM). Inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells (IC50 = 13 nM). Displays antinociceptive and analgesic effects in vitro; exhibits no significant sedative effect on locomotor activity.
Licensing Information
Sold with the permission of Astellas Pharma Inc.
Technical Data
| M. Wt | 360.52 |
| Formula | C19H28N4OS |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 446257-23-4 |
| PubChem ID | 11682007 |
| InChI Key | SASNRPJKZVJWQW-OAHLLOKOSA-N |
| Smiles | C1(NC4CCCCCC4)=C(C=C(CNC[C@H]3CCCO3)S2)C2=NC=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.05 | 100 | |
| ethanol | 36.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 360.52. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.77 mL | 13.87 mL | 27.74 mL |
| 5 mM | 0.55 mL | 2.77 mL | 5.55 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.77 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kohara et al (2007) Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models. Eur.J.Pharmacol. 571 8 PMID: 17597604
Satow et al (2008) Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allost J.Pharmacol.Exp.Ther. 326 577 PMID: 18487514
Keywords: YM 230888, supplier, YM230888, mGlu1, metabotropic, glutamate, receptors, group, I, 1, antagonist, antagonists, mGlu, selective, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
