Biological Activity
Potent and selective mGlu5 antagonist (IC50 values are 2.6 and 7.6 nM for rat and human receptors, respectively). Exhibits >3900-fold selectivity for mGlu5 over other mGlu receptors. Also selective over a panel of other targets. Displays discriminative effects in rats. Orally bioavailable and brain penetrant.
Compound Libraries
AZD 9272 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 284.22 |
| Formula | C14H6F2N4O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 327056-26-8 |
| PubChem ID | 9838729 |
| InChI Key | RBSPCALDSNXWEP-UHFFFAOYSA-N |
| Smiles | FC1=CC=C(C2=NOC(C3=CC(F)=CC(C#N)=C3)=N2)N=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 | 14.21 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 284.22. 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 | 3.52 mL | 17.59 mL | 35.18 mL |
| 5 mM | 0.7 mL | 3.52 mL | 7.04 mL |
| 10 mM | 0.35 mL | 1.76 mL | 3.52 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Swedberg and Raboisson (2014) AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J.Pharmacol.Exp.Ther. 350 212 PMID: 24876235
Raboisson et al (2012) Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg.Med.Chem.Lett. 22 6974 PMID: 23046966
Keywords: AZD 9272, supplier, AZD9272, mGlu5, antagonists, metabotropic, glutamate, receptors, orally, bioavailable, brain, penetrant, potent, selective, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
