UK 5099
| 中文名称 | UK 5099 |
|---|---|
| 中文同义词 | 2-氰基-3-(1-苯基-1H-吲哚-3-基)-2-丙烯酸;线粒体丙酮酸转运蛋白抑制剂(UK-5099);化合物UK5099;2-氰基-3-(1-苯基-1H-吲哚-3-基)丙烯酸;UK-5099,MCT抑制剂;UK 5099|||PF-1005023|||UK5099 |
| 英文名称 | 2-cyano-3-(1-phenylindol-3-yl)acrylate |
| 英文同义词 | 2-cyano-3-(1-phenylindol-3-yl)acrylate;PF-06340678;PF-1005023;2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid;UK 5099;(E)-2-cyano-3-(1-phenyl-1H-indol-3-yl)acrylic acid;Mitochondrial Pyruvate Carrier Inhibitor, UK5099;BIZNHCWFGNKBBZ-JLHYYAGUSA-N |
| CAS号 | 56396-35-1 |
| 分子式 | C18H12N2O2 |
| 分子量 | 288.3 |
| EINECS号 | |
| 相关类别 | 离子通道;膜转运;细胞生物学试剂;化工原料;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals |
| Mol文件 | 56396-35-1.mol |
| 结构式 |  |
UK 5099 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 | 二甲基亚砜：>20mg/mL |
| 酸度系数(pKa) | 1.49±0.19(Predicted) |
| 形态 | 粉末 |
| 颜色 | 黄色至棕褐色 |
| 稳定性 | 自购买之日起 1 年内保持稳定。 DMSO 或乙醇溶液可在 -20°C 下保存长达 1 个月。 |
| InChIKey | BIZNHCWFGNKBBZ-JLHYYAGUSA-M |
| Target | Value |
|
mitochondrial pyruvate carrier
() | 49 μM(Ki) |
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.
The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice.
安全信息
| WGK Germany | 3 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | XW5639635101 | 试剂UK 5099 UK 5099 | 25mg | 362元 | |
| 2024/04/30 | HY-15475 | UK 5099 UK-5099 | 56396-35-1 | 5mg | 650元 |