ROCK-IN-1HY-U00351-MedChemExpress

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ROCK-IN-1

型号：HY-U00351

产品价格：电议采购度：1737 原产地：中国大陆

发布时间：2018/5/18 23:52:18 所属地区：上海上海市

简要描述：

ROCK-IN-1 是一种有效的 ROCK 抑制剂，能够抑制 ROCK2 的活性，IC₅₀ 值为 nM。

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标签：ROCK-IN-1

产品详情

AZD 9272产品描述：AZD 9272 is a brain penetrant mGluR5 antagonist.IC50 & Target: mGluR5^{[1]^{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)^[1].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 t_1/2 of 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].
产品链接：www.medchemexpress.com/AZD_9272.html

研究领域：GPCR/G Protein

靶点：mGluR

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更新时间：2024/1/2 10:10:55}}

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