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.
Technical Data
| M. Wt | 588.67 |
| Formula | C22H30N4O2S.1.5C4H4O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 299900-84-8 |
| PubChem ID | 90488842 |
| InChI Key | HABHEZNVNBKOQJ-VQYXCCSOSA-N |
| Smiles | CN(CCOC)CC1=CC=C2C(N(C=C(C(N(C)C4CCCCC4)=O)S3)C3=N2)=C1.O=C(O)/C=C/C(O)=O.O=C(O)/C=C/C(O)=O.O=C(O)/C=C/C(O)=O.CN(CCOC)CC5=CC=C6C(N(C=C(C(N(C)C8CCCCC8)=O)S7)C7=N6)=C5 |
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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kohara et 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
Ferraguti et al (2008) Metabotropic glutamate 1 receptor: current concepts and perspectives. Pharmacol.Rev. 60 536 PMID: 19112153
Yanamoto et 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
