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AZD 9272
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产品介绍
产品介绍
产品信息
抗原名称
mGluR5 (rat):2.6±0.3 nM, mGluR5 (human):7.6±1.1 nM
商品描述
AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.
纯度
98%
可溶性
DMSO:12.8 mg/mL (45.0 mM)
In vitro(体外研究)
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(体内研究)
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]
背景
分子式
C14H6F2N4O
CAS号
327056-26-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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