GSK726701A|945721-87-9|-陌孚医药/Medlife

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GSK726701A

目录号: PL10109 纯度: ≥98%

CAS No. :945721-87-9

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中文名称	GSK726701A
英文名称	GSK726701A
英文别名	GSK726701A;2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)-2-fluorophenyl]acetic acid;BDBM50461449;{4-[4,9-Bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid;Chembl4229058;4-(4,9-Diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-2-fluorobenzeneacetic acid (ACI)
Cas No.	945721-87-9
分子式	C₂₄H₂₂FNO₅
分子量	423.43
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	GSK726701A是前列腺素E2受体4 (EP4)的部分激动剂，pEC₅₀为7.4。
生物活性	GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC 50 of 7.4.
性状	Solid
IC50 & Target[1][2]	pEC50: 7.4
体外研究(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 (pEC50=8.2) in a human whole blood (HWB) assay on the inhibition of LPS-mediated TNFα induction. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. 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]. Healy MP, et al. Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1892-1896.

溶解度数据	In Vitro: DMSO : 25 mg/mL (59.04 mM; Need ultrasonic)配制储备液

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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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