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AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.
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 |
Description | AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux. |
Targets&IC50 | mGluR5 (rat):2.6±0.3 nM, mGluR5 (human):7.6±1.1 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 | Shipping with blue ice. |
Solubility Information | DMSO: <1 mg/mL (insoluble or slightly soluble) |
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