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ONO-7300243研究进展
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服务商: 上海皓元生物医药科技有限公司 | 查看该公司所有服务 >> |
ONO-7300243产品描述:ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM. IC50 & Target: IC50: 0.19-0.13 μM (LPA1)[1] In Vitro: ONO-7300243 shows modest in vitro activity (IC50=0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro[1]. In Vivo: 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 公司介绍:MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库,总部位于美国新泽西,分别在瑞典和上海设有欧洲区子公司和亚洲区总代理,营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商, 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域,PI3K、MAPK等近千个细分靶点,超过4000个活性小分子化合物现货,以及GPCR、API、离子通道等超过20种不同类型的化合物库,同时提供从毫克到千克的专业定制合成服务。 MCE 对每批产品都进行严格的LCMS和NMR检验,其产品已被全球近万名客户广泛使用并发表大量文章、专利; MCE 定期增加各领域热门抑制剂、激动剂,不断扩增已有化合物库,以满足最新的科研需求; 数千种产品在上海有充足备货,24-48小时内送达客户; 大量产品提供免费试用装; 已为全球多个知名企业、院校构建各种定制型化合物库。 产品链接:www.medchemexpress.cn/ono-7300243.html src="http://img.dxycdn.com/trademd/upload/userfiles/image/2014/08/A1408605159png_small.jpg" alt=""> |