Fig. 1 · Structure

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AZD 9272

mGluR5 antagonist

AZD 9272 is a brain penetrant mGluR5 antagonist.

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Biological Activity

Target & Activity

Target Activity Value
mGluR5  

Cellular Effect

Cell Line Activity Value Description Reference
HEK293 IC50 2.6 nM Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay [PMID: 23046966]
HEK293 IC50 26 nM Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of glutamate-stimulated IP accumulation incubated for 10 mins prior to glutamate challenge measured 30 mins post glutamate challen [PMID: 23046966]
HEK293 IC50 7.6 nM Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay [PMID: 23046966]

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 327056-26-8
Applications mGluR5 antagonist
Formula C14H6F2N4O
Molecular Weight 284.22
SMILES
N#CC1=CC(F)=CC(C2=NC(C3=CC=C(F)C=N3)=NO2)=C1

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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