AZD 9272

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Cat.No. 5613 - AZD 9272 | C14H6F2N4O | CAS No. 327056-26-8
Description: Potent and selective mGlu5 antagonist; brain penetrant
Chemical Name: 3-Fluoro-5-[3-(5-fluoro-2-pyridinyl)-1,2,4-oxadiazol-5-yl]benzonitrile
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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

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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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Keywords: AZD9272 mGlu5 antagonists metabotropic glutamate receptors orally bioavailable brain penetrant potent selective Glutamate (Metabotropic) Group I Receptors

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