Description: High affinity, selective mGlu1 antagonist
Chemical Name:N-Cyclohexyl-6-[[N-(2-methoxyethyl)-N-methylamino]methyl]-N-methylthiazolo[3,2-a]benzoimidazole-2-carboxamide sesquifumarate
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
High affinity, selective metabotropic glutamate receptor type 1 (mGlu1) antagonist. Binds an allosteric site of the rat mGlu1 receptor with a Ki of 4.8 nM. Inhibits mGlu1-mediated inositol phosphates production (IC50 = 8.6 nM in rat cerebellar granule cells). Neuroprotective in vivo.
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
48.75
100
water
9.75
20
Preparing Stock Solutions
The following data is based on the product molecular weight 588.67. 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
1.7 mL
8.49 mL
16.99 mL
5 mM
0.34 mL
1.7 mL
3.4 mL
10 mM
0.17 mL
0.85 mL
1.7 mL
50 mM
0.03 mL
0.17 mL
0.34 mL
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
Select another language:
View SDS
References
References are publications that support the products' biological activity.
Koharaet al (2008) Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models. Brain Res. 1191 168 PMID: 18164695
Ferragutiet al (2008) Metabotropic glutamate 1 receptor: current concepts and perspectives. Pharmacol.Rev. 60 536 PMID: 19112153
Yanamotoet al (2010) Radiosynthesis and evaluation of [11C]YM-202074 as a PET ligand for imaging the metabotropic glutamate receptor type 1. Nucl.Med.Biol. 37 615 PMID: 20610166
Keywords: YM 202074, supplier, selective, YM202074, YM, 202074, sesquifumarate, metabotropic, glutamate, receptors, antagonists, mGluR1, mGlu, mGlu1, Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience