7-（（R）-2-（（3S，4S，E）-3-hydroxy-4-methylnon-1-en-6-yn-1-yl）-5-氧吡咯烷-1--1-基）庚酸-7-((R)-2-((3S,4S,E)-3-hydroxy-4-methylnon-1-en-6-yn-1-yl)-5-oxopyrrolidin-1-yl)heptanoic acid代理/参数/厂家-生化试剂-艾美捷科技有限公司

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中文名称: 7-（（R）-2-（（3S，4S，E）-3-hydroxy-4-methylnon-1-en-6-yn-1-yl）-5-氧吡咯烷-1--1-基）庚酸

英文名字: 7-((R)-2-((3S,4S,E)-3-hydroxy-4-methylnon-1-en-6-yn-1-yl)-5-oxopyrrolidin-1-yl)heptanoic acid

背景资料: The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 (PGE2; Item No. 14010). Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619,24126} KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 (Item No. 13010) that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors).{25026} In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK-293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively.{25026} KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 (Item No. 10007712) is highly cytotoxic at similar concentrations in these cells.{25027} KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.{25027}

产品描述: A selective, potent agonist of EP4 with an IC50 value of 3 nM (versus 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors) and an EC50 value of 0.19 nM in functional assays; induces the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively); repairs calvarial defects in an in vivo rat craniomaxillofacial reconstruction model and promotes bone formation in a rat incisor tooth socket model

其他: Cayman Chemical向全球科学工作者提供多研究领域的生化、免疫试剂和分析试剂盒，其产品被广泛应用于肿瘤、氧化氮、神经学、凋亡、氧化性损伤、内分泌学等不同研究领域.Cayman Chemical可提供用于检测的特色试剂盒，如：类花生酸类物质、游离的生物标志、环核苷、激素及氧化氮等；也提供多种高质量试剂，包括：类花生酸类物质、氧化氮试剂及许多相关脂质、脂肪酸、酶和抗体.作为Cayman Chemical在中国的区域总代理，艾美捷科技有限公司将为中国客户提供最全面的Cayman Chemical产品以及客户订制化服务.