AZD-9272
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1020 | To Be Confirmed |
| 500mg | $1480 | To Be Confirmed |
| 1g | $2220 | To Be Confirmed |
: Cat #: V4351 CAS #: 327056-26-8 Purity ≥ 98%
Description: AZD-9272 is a potent, selective, orally bioavailable and brain penetrant antagonist mGlu5 (metabotropic glutamate receptor 5) with IC50 values of 2.6 and 7.6 nM for rat and human receptors, respectively.
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| Molecular Weight (MW) | 284.22 |
|---|---|
| Molecular Formula | C14H6F2N4O |
| CAS No. | 327056-26-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent |
| Protocol | In Vitro | AZD 9272 causes a concentration dependent decrease in the magnitude of the intracellular Ca2+ response to 1.5 μM of the mGluR group I selective agonist DHPG in both the human and the rat mGluR5 expressing cell lines. The maximal inhibition is 100%. The mean IC50 (±SD) value at the human mGluR5 is 7.6±1.1 nM (n=13) for AZD9272. The mean IC50 value at the rat mGluR5 is 2.6±0.3 nM (n=3) for AZD9272. In contrast, 10 μM of AZD9272 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. 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). |
|---|---|---|
| In Vivo | The clearance of AZD 9272 is low following a single intravenous dose at 3 μmol/kg and AZD 9272 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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.5184 mL | 17.5920 mL | 35.1840 mL | 70.3680 mL |
| 5mM | 0.7037 mL | 3.5184 mL | 7.0368 mL | 14.0736 mL |
| 10mM | 0.3518 mL | 1.7592 mL | 3.5184 mL | 7.0368 mL |
| 20mM | 0.1759 mL | 0.8796 mL | 1.7592 mL | 3.5184 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
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PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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