计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC 50 of 7.4.
In Vitro
GSK726701A has high selectivity (>100-fold) against a set of other prostaglandin receptors (EP1-3 , DP1 , FP, IP, TP) and no significant activity against a wider panel of targets. It demonstrates EP4 agonist activity with similar potency and intrinsic activity (pEC 50 =8.2) in a human whole blood (HWB) assay on the inhibition of LPS-mediated TNFα induction. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GSK726701A has good pharmacokinetic file in rat, dog and monkey. GSK726701A has robust activity in a range of animal models of inflammatory and neuropathic pain GSK726701A demonstrates a time-dependant, full reversal of CCI-induced mechanical allodynia at 3mg/kg, equivalent to the clinical gold standard gabapentin (30mg/kg). GSK726701A has an ED 50 of 0.2mg/kg in the FCA acute rat model of inflammatory pain . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:pEC50: 7.4