UK 5099

UK 5099化学性质

熔点 :235-238°C
沸点 :448.6±45.0 °C(Predicted)
密度 :1.20
储存条件 :2-8°C
溶解度 :DMSO: >20mg/mL
酸度系数(pKa) :1.49±0.19(Predicted)
形态 :powder
颜色 :yellow to tan
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
InChIKey :BIZNHCWFGNKBBZ-JLHYYAGUSA-M

安全信息

UK 5099性质、用途与生产工艺

生物活性 UK-5099 (PF-1005023) 是线粒体丙酮酸转运蛋白 (MPC) 的有效抑制剂，抑制丙酮酸依赖性O2消耗的 IC50 值为50 nM。
靶点
Target Value
mitochondrial pyruvate carrier
() 49 μM(Ki)
体外研究

The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (K _i =17 mM) but can be completely blocked by UK-5099 (K _i =49 microM). UK-5099 also inhibits the monocarboxylate transporter (MCT) . UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal model for Warburg effect studies.
体内研究

The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice.

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UK 5099生产厂家

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Target	Value
mitochondrial pyruvate carrier ()	49 μM(Ki)