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Tocris/AZD 9272/5613/10/10 mg

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货号: 5613/10

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

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
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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

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

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