中文名 | 2-氰基-3-(1-苯基-1H-吲哚-3-基)-2-丙烯酸 |
英文名 | 2-cyano-3-(1-phenylindol-3-yl)acrylate |
别名 | 化合物UK5099 线粒体丙酮酸转运蛋白抑制剂 线粒体丙酮酸转运蛋白抑制剂(UK-5099) 2-氰基-3-(1-苯基-1H-吲哚-3-基)丙烯酸 2-氰基-3-(1-苯基-1H-吲哚-3-基)-2-丙烯酸 |
英文别名 | UK 5099 PF-1005023 PF-06340678 BIZNHCWFGNKBBZ-JLHYYAGUSA-N 2-cyano-3-(1-phenylindol-3-yl)acrylate Mitochondrial Pyruvate Carrier Inhibitor, UK5099 (E)-2-cyano-3-(1-phenyl-1H-indol-3-yl)acrylic acid 2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid |
CAS | 56396-35-1 |
化学式 | C18H12N2O2 |
分子量 | 288.3 |
InChIKey | BIZNHCWFGNKBBZ-JLHYYAGUSA-M |
密度 | 1.20 |
熔点 | 235-238°C |
沸点 | 448.6±45.0 °C(Predicted) |
溶解度 | DMSO: >20 mg/mL |
酸度系数 | 1.49±0.19(Predicted) |
存储条件 | 2-8°C |
稳定性 | 从提供的购买之日起稳定1年。DMSO或乙醇中的溶液可以在-20 °C下储存长达1个月。 |
外观 | 粉末 |
颜色 | yellow to tan |
物化性质 | 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。 |
MDL号 | MFCD19443867 |
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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.469 ml | 17.343 ml | 34.686 ml |
5 mM | 0.694 ml | 3.469 ml | 6.937 ml |
10 mM | 0.347 ml | 1.734 ml | 3.469 ml |
5 mM | 0.069 ml | 0.347 ml | 0.694 ml |
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