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AZD 9272

AZD 9272
AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.
Catalog No. T14389Cas No. 327056-26-8
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Purity:97.53%
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AZD 9272

Purity: 97.53%
Catalog No. T14389Cas No. 327056-26-8

AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$42In Stock
5 mg$98In Stock
10 mg$158In Stock
25 mg$355In Stock
50 mg$533In Stock
100 mg$783In Stock
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Product Introduction

Bioactivity
Description
AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.
Targets&IC50
mGluR5 (human):7.6±1.1 nM, mGluR5 (rat):2.6±0.3 nM
In vitro
AZD9272 (10 μM) does not diminish the response to 10 μM ATP in the background GHEK cells. Increasing concentrations of AZD9272 causes a decrease in the potency and the maximal response of DHPG.[1] AZD9272 completely reverses the glutamate-stimulated (EC80=80 μM) phosphatidyl inositol hydrolysis in human mGluR5-GHEK cells in a concentration-dependent manner, with IC50 of 26±3 nM (n=21).[1]
In vivo
AZD 9272 (3 μmol/kg; single intravenous) is eliminated from plasma with terminal half-lives between 2 and 6 h. The terminal half-lives following oral dosing are similar to the half-lives following intravenous dosing. The volume of distribution at steady state is intermediate for AZD9272.[1]
AZD9272 (2.84 mg/kg) causes greater than 80% and typically more than 99% MTEP-appropriate responding up to 20 hours after dose, with a decline to approximately 20% at 24 hours after dose, yielding a t1/2 of 21.93 hours, and causes no systematic effects on response rates. The first-time point at which AZD9272 causes >90% MTEP-appropriate response is at 30 minutes after the dose.[2]
Chemical Properties
Molecular Weight284.22
FormulaC14H6F2N4O
Cas No.327056-26-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: <1 mg/mL (insoluble or slightly soluble)

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