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首页 制药产品大全 原料药 激素及调节药原料 依帕列净

依帕列净

2026-02-27
864070-44-0
中国药典,美国药典,英国药典,欧洲药典,日本药典,企业标准
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产品详情

依帕列净
激素类
864070-44-0
中国药典,美国药典,英国药典,欧洲药典,日本药典,企业标准
药用级
北美洲,中/南美洲,西欧,东欧,大洋洲,亚洲,中东,非洲

产品描述

描述:Empagliflozin是一种选择性钠葡萄糖协同转运蛋白-2 (SGLT-2) 抑制剂,抑制人SGLT-2的IC50 为3.1 nM

相关类别:

信号通路 >> 跨膜转运 >> SGLT

研究领域 >> 代谢疾病

靶点:IC50: 3.1 nM (SGLT-2), 1.1 μM (SGLT-5), 2 μM (SGLT-6), 8.3 μM (SGLT-1), 11 μM (SGLT-4)

体外研究:Empagliflozin是一种有效且具有竞争力的SGLT-2抑制剂,具有优异的选择性和测试的SGLT-2抑制剂相对于hSGLT-1的最高选择性窗口。 Empagliflozin以剂量依赖性方式通过hSGLT-2抑制[14 C]-α-甲基吡喃葡萄糖苷(AMG)的摄取,IC50为3.1 nM,但对其他SGLT的效力较低(IC50范围:1100-11000nM)。在动力学结合实验中,[3H] -Empagliflozin对SGLT-2表现出高亲和力,在没有葡萄糖的情况下平均Kd为57±37nM

体内研究:在任一剂量的Empagliflozin处理8天后,葡萄糖不耐受显着改善(3mg / kg Empagliflozin 3058±180对10mg / kg Empagliflozin 3090±219)。因此,Empagliflozin的急性治疗对高血糖和葡萄糖耐受不良有益。由于两种不同剂量的Empagliflozin血糖稳态无显着差异,并且3mg / kg Empagliflozin显着改善T1DM小鼠的随机血糖水平,因此较低剂量的Empagliflozin(3mg / kg)的作用是研究保留β细胞的质量和功能

激酶实验:在存在或不存在20mM葡萄糖的情况下,在含有137mM NaCl的10mM 4-(2-羟乙基)-1-哌嗪乙磺酸(HEPES)缓冲液(pH7.4)中测定膜(60μg/孔),并指示浓度为[3H] -Empagliflozin在96孔板中在室温下保持2小时。通过用0.5%聚乙烯亚胺浸渍的GF / B滤板快速过滤来终止孵育,并用0.9%NaCl溶液预润湿,并使用Harvester Filtermate 96用0.9%NaCl溶液(4℃)洗涤四次。将滤板干燥2小时每孔加入50μLMicroscint20。使用TopCount NXT测量保留在过滤器上特性。同时,通过在配体结合研究中将每孔加入的相同量的[3H] - 伊曲利嗪和4mL Ultima Gold Scintilator加入到5mL小瓶中并使用Tricarb测量来确定测定中使用的实际活性量。 2900TR。在30μM达格列嗪[1]存在下测定非特异性[3H] -Empagliflozin结合

动物实验:小鼠[2]使用雄性C57BL / 6J小鼠(10周龄)。将依帕列净溶于羟乙基纤维素(HEC)中,并通过口服管饲法每天一次给予实验组(3或10mg / kg)的小鼠8天,而赋形剂组仅给予相同体积的HEC

密度:1.4±0.1 g/cm3

沸点:664.5±55.0 °C at 760 mmHg

分子式:C23H27ClO7

分子量:450.909

闪点:355.7±31.5 °C

精确质量:450.144531

PSA:108.61000

LogP:3.38

蒸气压:0.0±2.1 mmHg at 25°C

折射率:1.628

 

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中文简介: 深圳天缘医药科技有限公司,是一家致力于为全球医药行业提供全方位服务的高科技企业。自成立以来,我们始终坚持以科技创新为核心,以满足客户需求为导向,为全球医药企业提供从药物发现到生产过程的一体化解决方案。我们的业务范围覆盖了药物研发、生产、销售、技术支持等多个领域,为客户提供全方位的服务支持。   我们的研发团队拥有世界一流的科研实力,汇集了众多国内外的药物研发专家和技术骨干。在药物研发过程中,我们秉持创新、高效、安全的原则,采用先进的技术手段和设备,充分发挥团队的专业优势,为客户提供高质量的药物研发服务。在生物药物的研发和生产过程中,我们采用了一系列创新技术和方法,有效地简化了生产流程,提高了生产效率,降低了生产成本,为客户带来了显著的经济效益。   我们的质量管理体系已通过FDA(美国食品药品监督管理局)、EMA(欧洲药品管理局)和NMPA(国家药品监督管理局)的认证,充分体现了我们在质量管理方面的严谨态度和高标准要求。为了更好地服务客户,我们在深圳前海自贸区投资建设了一座多功能医药研发中心,提供从药物筛选、药物设计、药物合成、药物评价等全过程的一站式服务。   在治疗重大疾病领域,我们取得了一系列令人瞩目的成果。在抗病毒、肿瘤、代谢、心血管等领域,我们凭借强大的研发实力和丰富的行业经验,为全球医药企业研发了众多高效、安全的创新药物。尤其在替尼药物方面,我们拥有无与伦比的能力和专业知识,为全球医药企业提供了高质量的替尼药物研发服务。   作为一家国际化的医药科技企业,我们与全球3200多家合作伙伴建立了良好的合作关系,为客户提供了全球范围内的业务支持和服务。在商业化药物开发过程中,我们始终坚持“真正的一站式”理念,为客户提供从药物研发、生产、销售到技术支持等全方位的服务,帮助客户实现药物的快速上市和商业化。   展望未来,深圳天缘医药科技有限公司将继续坚持创新驱动、科技领先的发展战略,加大研发投入,不断提升技术水平和服务质量,为全球医药行业的发展做出更大的贡献。我们将与全球合作伙伴共同努力,为人类健康事业的发展贡献智慧和力量,为创造美好的未来而不懈努力。   英文简介: Shenzhen Tianyuan Pharmaceutical Technology Co., Ltd. is a high-tech enterprise dedicated to providing a full range of services for the global pharmaceutical industry. Since its inception, we have always adhered to scientific and technological innovation as the core, to meet customer needs as the orientation, to provide global pharmaceutical companies with integrated solutions from drug discovery to production process. Our business scope covers drug research and development, production, sales, technical support and other areas, to provide customers with a full range of service support. Our R & D team has world-class scientific research strength and brings together many top drug R & D experts and technical backbones at home and abroad. In the process of drug research and development, we adhere to the principles of innovation, efficiency and safety, adopt advanced technical means and equipment, give full play to the professional advantages of the team, and provide customers with high-quality drug research and development services. In the process of R & D and production of biopharmaceuticals, we have adopted a series of innovative technologies and methods to effectively simplify the production process, improve production efficiency, reduce production costs, and bring significant economic benefits to customers. Our quality management system has been certified by FDA (US Food and Drug Administration), EMA (European Drug Administration) and NMPA (State Drug Administration), which fully reflects our stringent attitude and high standards in quality management. In order to better serve our customers, we have invested in building a multi-functional pharmaceutical R & D center in Qianhai Free Trade Zone in Shenzhen, providing one-stop services for the whole process of drug screening, drug design, drug synthesis, drug evaluation and so on. In the field of treating major diseases, we have made a series of remarkable achievements. With our strong R & D strength and rich industry experience, we have developed many efficient and safe innovative drugs for global pharmaceutical companies in the fields of antiviral, oncology, metabolism, cardiovascular and so on. Especially in the field of tini drugs, we have unparalleled ability and expertise to provide high-quality tini drug research and development services for global pharmaceutical companies. As an international pharmaceutical technology enterprise, we have established a good cooperative relationship with more than 3200 partners around the world to provide customers with global business support and services. In the process of commercial drug development, we always adhere to the "real one-stop" concept, providing customers with a full range of services from drug research and development, production, sales to technical support, to help customers achieve rapid drug marketing and commercialization. Looking to the future, Shenzhen Tianyuan Pharmaceutical Technology Co., Ltd. will continue to adhere to the innovation-driven and technology-leading development strategy, increase R & D investment, constantly improve the technical level and service quality, and make greater contributions to the development of the global pharmaceutical industry. We will make joint efforts with global partners to contribute wisdom and strength to the development of human health and make unremitting efforts to create a better future.   关键词: 英文:Filgotinib maleate,Pralsetinib (BLU-667),Pemigatinib,TIC10,Sodium phenylbutyrate,Mirogabalin besylate,Tyk2-IN-4(BMS986165),Ribociclib,Dotinurad,2,6-Bis(hydroxymethyl)-p-cresol,Brincidofovir,Finerenone,Peficitinib,Ticagrelor,Vonoprazan Fumarate (TAK-438),Sacubitril/valsartan (LCZ696),Upadacitinib,Tofacitinib (CP-690550) Citrate               中文: 非戈替尼、拉西替尼(BLU-667)、培米加替尼、onc201(TIC10)、4-苯基丁酸钠盐、米洛巴林、氘可来替尼(BMS-986165)、瑞博西尼(LEE011)、多替诺德、布罗福韦酯(CMX001)、2-羟基-5-甲基间苯二甲醇、非奈利酮、培菲替尼、替卡格雷、富马酸沃诺拉赞、沙卡布曲缬沙坦(LCZ696)、乌帕替尼、托法替尼  
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