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AZD 9272
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD 9272图片
CAS NO:327056-26-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
AZD 9272 是一种脑渗透性mGluR5拮抗剂。
生物活性

AZD 9272 is a brain penetrantmGluR5antagonist.

IC50& Target[1]

mGluR5

 

体外研究
(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 IC50value 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 IC50of 26±3 nM (n=21)[1].

体内研究
(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[1]. AZD9272 causes no cocaine-appropriate responding and causes a non-dose-dependent reduction in response rates at higher doses. AZD9272 at 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 t1/2of 21.93 hours, and causes no systematic effects on response rates. The first time point at which AZD9272 causes >90% MTEP-appropriate responding is at 30 minutes after dose[2].

分子量

284.22

Formula

C14H6F2N4O

CAS 号

327056-26-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.