当前位置: 首页 » 资讯 » 行业动态 » 正文

AMG 837 (calcium hydrate)研究进展

发布日期：2017-11-02   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/AMG-837-calcium-hydrate.htmlAMG 837 (calcium hydrate)/a产品描述：AMG 837 calcium h
AMG 837 (calcium hydrate)产品描述：AMG 837 calcium hydrate is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ.  An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly


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/amg-837-calcium-hydrate.html