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ONO-7300243研究進(jìn)展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/ONO-7300243.htmlONO-7300243/a產(chǎn)品描述：ONO-7300243 is a novel, potent lysophosphat
<a href="https://www.medchemexpress.com/ONO-7300243.html">ONO-7300243</a>產(chǎn)品描述：ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (<b>LPA1</b>) antagonist with <b>IC<sub>50</sub></b> of 0.16 μM.

IC50 & Target: IC50: 0.19-0.13 μM (LPA1)<sup>[1]</sup>

<i><b>In Vitro:</b></i> ONO-7300243 shows modest in vitro activity (IC<sub>50</sub>=0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro<sup>[1]</sup>.

<i><b>In Vivo:</b></i> ONO-7300243 shows good efficacy in vivo. The oral dosing of 17a at 30 mg/kg leads to reduced intraurethral pressure in rats. ONO-7300243 shows stronge effects in vivo (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.) compared with compound 12g. The results reveal that ONO-7300243 shows good membrane permeability and good metabolic stability against rat liver microsomes (MS). ONO-7300243 exhibits good selectivity towards LPAl over LPA2, most likely because low molecular weight and low lipophilicity lead to reduced compound promiscuity and increased selectivity. ONO-7300243 inhibit<br><br>
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已為全球多個(gè)知名企業(yè)、院校構(gòu)建各種定制型化合物庫(kù)。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/ono-7300243.html">www.medchemexpress.cn/ono-7300243.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

src="http://img.dxycdn.com/trademd/upload/userfiles/image/2014/08/A1408605159png_small.jpg"

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