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AZD 9272

Catalog No. T14389   CAS 327056-26-8

AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.

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AZD 9272 Chemical Structure
AZD 9272, CAS 327056-26-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 89.00
5 mg In stock $ 192.00
10 mg In stock $ 297.00
25 mg In stock $ 596.00
50 mg In stock $ 848.00
100 mg In stock $ 1,170.00
500 mg In stock $ 2,350.00
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Purity: 97.53%
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Biological Description
Chemical Properties
Storage & Solubility Information
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]
Molecular Weight 284.22
Formula C14H6F2N4O
CAS No. 327056-26-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.8 mg/mL (45.0 mM)

TargetMolReferences and Literature

1. Swedberg MD, et al. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J Pharmacol Exp Ther. 2014 Aug;350(2):212-22. 2. Raboisson P, et al. Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6974-9.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

AZD 9272 327056-26-8 Neuroscience GluR AZD9272 AZD-9272 inhibitor inhibit

 

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