MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 1564265-82-2
MCE 国际站:PS10
产品活性:PS10 是一种新型,有效且具有 ATP 竞争性的广谱 PDK 抑制剂,可抑制所有 PDK 同工型,对 PDK2,PDK4,PDK1 和 PDK3 的 IC50 分别为 0.8 μM,0.76 μM,2.1 μM 和 21.3 μM。 PS10 对 PDK2 (Kd= 239 nM) 的亲和力高于对 Hsp90 (Kd= 47 μM)。 PS10 改善葡萄糖耐量,刺激饮食引起的肥胖症中的心肌碳水化合物氧化。 PS10 具有研究糖尿病性心肌病的潜力。
研究领域:Metabolic Enzyme/Protease
作用靶点:PDHK
In Vitro: PS10 shows a higher affinity of PS10 for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47,000 nM).PS10 is less potent than cycloheximide in HeLa cells, it shows an IC50 value of 284 μM for the growth inhibition and PS10 has low toxicity in cells.
In Vivo: PS10 (Intraperitoneal injection; 70 mg/kg; single dose) treatment lead to 11- and 23-fold higher PDC activity in heart and liver, respectively. Meanwhile, there results in a 1.4-fold enhancement of PDC activity in kidneys compared with vehicle-group.PS10 (Intraperitoneal injection; 70 mg/kg; 3 days) treatment results that thePDC activity profiles and the phospho-E1α subunit level is similar to the single-dose. Notably, the three-day treatment attenuates the enhancement of PDK activity in heart.PS10 (intraperitoneal injection; 70 mg/kg; 4 weeks) is treated in mice and subjected to a glucose tolerance test. when challenged with 1.5 g/kg glucose, the plasma glucose level in the vehicle-treated control is at 200 mg/dl at 0 min, peaks at 482 mg/dl at 30 min, and reduces to 210 mg/dl at 120 min. In PS10-treated DIO mice, the glucose level at 168 mg/dl at 0 min is lower than that in vehicle-treated animals, reachs 312 mg/dl at 30 min, and returns to 163 mg/dl at 120 min.PS10 (intraperitoneal injection; 70 mg/kg) and DCA both stimulates flux through PDC as measured by the appearance of hyperpolarized [13C]bicarbonate. It shows similar glucose tolerance response to glucose challenge restores PDC activity in the DIO mouse hearts.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | Metabolism/Protease Compound Library | Anti-diabetic Compound Library | Glycolysis Compound Library | Anti-Cancer Metabolism Compound Library | Mitochondria-Targeted Compound Library | Glucose Metabolism Compound Library | Targeted Diversity Library | TCA Cycle Compound Library | AZD7545 | VER-246608 | PDHK-IN-3 | TM-1 | PDK4-IN-1 hydrochloride | KPLH1130 | PDHK-IN-5 | Leelamine | PDK-IN-1 | M77976 | JX06 | Dicoumarol | PDHK-IN-4 | Sodium dichloroacetate
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-121744
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。