Biological Activity
Non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM); inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). Inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively), and is orally active in vivo, demonstrating an antinociceptive effect in hyperalgesic mice. Desmethyl derivative (Cat. No. 2447) also available.
Licensing Information
Sold with the permission of Astellas Pharma Inc.
Technical Data
| M. Wt | 378.92 |
| Formula | C18H22N4OS.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1216398-09-2 |
| PubChem ID | 45073464 |
| InChI Key | WYTJVUVCSUWZTH-UHFFFAOYSA-N |
| Smiles | Cl.CN(C1CCCCC1)C(=O)C1=C(C)N2C(S1)=NC1=CC=C(N)C=C21 |
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 | |||
| water | 37.89 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 378.92. 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 | 2.64 mL | 13.2 mL | 26.39 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.28 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Kohara et al (2005) Radioligand binding properties and pharmacological characterization of 6-Amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]-benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective and noncompetitive antagonist of metabo J.Pharmacol.Exp.Ther. 315 163 PMID: 15976016
Emery et al (2010) The protective signaling of metabotropic glutamate receptor 1 is mediated by sustained, β-arrestin-1-dependent ERK phosphorylation. J.Biol.Chem. 285 26041 PMID: 20566651
Keywords: YM 298198 hydrochloride, supplier, potent, selective, non-competitive, mGlu1, mGluR1, antagonists, Group, I, Receptors, Glutamate, Metabotropic, YM298198, hydrochloride, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
