Biological Activity
Selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively). Reduces hyperalgesic behavior induced by formalin in both mouse and rat with ED50 values of 28 and 16.3 mg/kg respectively.
Compound Libraries
LY 456236 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 317.77 |
| Formula | C16H15N3O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 338736-46-2 |
| PubChem ID | 9926998 |
| InChI Key | AVKFOWUSTVWZQN-UHFFFAOYSA-N |
| Smiles | Cl.COC1=CC=C(NC2=C3C=C(OC)C=CC3=NC=N2)C=C1 |
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 | 6.36 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 317.77. 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 | 3.15 mL | 15.73 mL | 31.47 mL |
| 5 mM | 0.63 mL | 3.15 mL | 6.29 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.15 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Shannon et al (2005) Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology 49 188 PMID: 16011839
Bertorelli et al (2005) Selective blockade of metabotropic glutamate subtype mGluR1 receptors induce anti-nociceptive effects. Neuropharmacology 49 231 PMID:
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