化合物UK5099 T4441
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 56396-35-1 | ¥538.00 | 询底价 |
2 mg | 56396-35-1 | ¥329.00 | 询底价 |
1 mg | 56396-35-1 | ¥233.00 | 询底价 |
100 mg | 56396-35-1 | ¥4,250.00 | 询底价 |
50 mg | 56396-35-1 | ¥2,590.00 | 询底价 |
25 mg | 56396-35-1 | ¥1,560.00 | 询底价 |
1 mL | 56396-35-1 | ¥563.00 | 询底价 |
10 mg | 56396-35-1 | ¥828.00 | 询底价 |
Product Introduction
Bioactivity
英文名: UK-5099
描述: UK-5099 (PF-1005023) 是一种有效的线粒体丙酮酸转运蛋白(MPC) 抑制剂, 抑制丙酮酸依赖性 O2消耗的 IC50值为50 nM。
细胞实验: The 832/13 cell line derived from INS-1 rat insulinoma cells is used for experiments. Cell viability is measured using CellTiter Blue. The assay is based on the cellular reduction of resazurin to resorufin. The appearance of resorufin is monitored by fluorescence emission at 585 nm using a Spectramax M5 microplate reader with excitation at 555 nm. For UK5099-treated cells, cells are allowed to recover for 1 h before measuring cell viability. Data are expressed as -fold relative to no treatment or siCtrl[4].
动物实验: C57BLK mice are fasted for 16 h prior to glucose challenge. UK5099 (32 μmol/kg of body weight) or DMSO in PBS is injected into the intraperitoneal cavity 30 min before injecting glucose (1.5 mg of glucose/g of body weight). Blood glucose levels are measured at 0, 10, 20, 30, 60, and 120 min after glucose injection[4].
体外活性: The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki: 17 mM) but can be completely blocked by UK-5099 (Ki: 49 μM)[2]. UK-5099 also inhibits the monocarboxylate transporter (MCT) [3]. UK5099 dose-dependently significantly inhibits the glucose-stimulated rise in oxygen consumption and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells[4]. The UK5099 treated cells show a significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. The UK5099 application may be an ideal model for Warburg effect studies[5].
体内活性: UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice[4].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: 5% DMSO+95% Saline : 1.44 mg/mL (4.99 mM, suspension)
DMSO : 16.67 mg/mL (57.81 mM)
关键字: Mitochondrial Metabolism | inhibit | UK-5099 | PF 1005023 | Inhibitor | PF1005023
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相关库: Anti-Aging Compound Library | Glycometabolism Compound Library | Mitochondria-Targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Cuproptosis Compound Library | Reprogramming Compound Library | NO PAINS Compound Library | Covalent Inhibitor Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途