GSK-269984A
目录号: PL10139 纯度: ≥99%
CAS No. :892664-04-9
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中文名称
GSK-269984A
英文名称
GSK-269984A
英文别名
GSK-269984A;sodium,6-[[5-chloro-2-[(4-chloro-2-fluorophenyl)methoxy]phenyl]methyl]pyridine-2-carboxylate
Cas No.
892664-04-9
分子式
C20H13NO3FCl2-.Na+
分子量
428.22
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GSK-269984A 是前列腺素 E2 受体 1 (Prostaglandin E2 Receptor 1 (EP1)) 的拮抗剂,pIC50 值为 7.9。
生物活性
GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC 50 of 7.9.
性状
Solid
IC50 & Target[1][2]
pIC50: 7.9 (Prostaglandin E2 Receptor 1 (EP1))
体外研究(In Vitro)
Results from [H]-PGE2 binding assay in CHO cells overexpressing the human EP1 receptor demonstrate that GSK-269984A is an antagonist of EP1 receptor with a pIC50 of 7.9. GSK-269984A is found to cause a concentration-dependent rightward shift of the PGE2 dose-response curve and Schild analysis shows that GSK-269984A is a competitive antagonist with pA2 8.1±0.3 and slope 1.0. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GSK-269984A demonstrates an ED 50 of 2.6 mg/kg (po), with the 10 mg/kg dose showing equivalent reversal of hypersensitivity to the standard. GSK-269984A displays moderate blood clearance in the rat and dog and high clearance in the monkey which is reflected in the half-life for each species. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Hall A, et al. Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain. Bioorg Med Chem Lett. 2009 May 1;19(9):2599-603.
溶解度数据
In Vitro: DMSO : 7 mg/mL (16.31 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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