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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
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $42 | In Stock | |
| 5 mg | $98 | In Stock | |
| 10 mg | $158 | In Stock | |
| 25 mg | $355 | In Stock | |
| 50 mg | $533 | In Stock | |
| 100 mg | $783 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| Storage | Powder: -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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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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