YM 298198 hydrochloride

Cat. No. 2448

YM 298198 hydrochloride C18H22N4OS.HCl [1216398-09-2]

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Chemical Name: 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide hydrochloride

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
Solubility:
Soluble to 100 mM in water
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
1216398-09-2

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

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.

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 metabotropic glutamate receptor type 1. J.Pharmacol.Exp.Ther. 315 163. PMID: 15976016.

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Keywords: YM 298198 hydrochloride, supplier, potent, selective, non-competitive, mGlu1, mGluR1, antagonists, Group, I, Receptors, Glutamate, Metabotropic, YM298198, hydrochloride, Tocris Bioscience, Glutamate (Metabotropic) Group I Receptor Antagonist products

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