| CAS NO: | 56396-35-1 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 288.3 |
| Cas No. | 56396-35-1 |
| Formula | C18H12N2O2 |
| Synonyms | PF-1005023;UK5099;UK 5099;PF1005023;PF 1005023 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥28.8 mg/mL in DMSO |
| Chemical Name | (E)-2-cyano-3-(1-phenylindol-3-yl)prop-2-enoic acid |
| Canonical SMILES | C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
UK-5099是一种强效的线粒体丙酮载体抑制剂[1]。
线粒体丙酮载体(MPC)协助丙酮酸盐穿过线粒体内膜转运，并在碳水化合物、脂质和氨基酸代谢中起关键作用。
UK-5099 (1 mM)完全阻断丙酮酸盐摄取，Ki值为49 μM。同时，UK-5099浓度依赖性地减少总的外流率[ 1 ]。在分离自S. Guttatum的线粒体中，UK-5099 (20 μM)抑制丙酮酸盐依赖型02的消耗[ 2 ]。
在大鼠心脏线粒体中，UK-5099 抑制丙酮酸氧化作用，其具有非线性的阻抑动力学[ 2 ]。在胰高血糖素处理过的大鼠中，UK-5099 呈线性关系地抑制丙酮酸羧化反应和全部丙酮酸代谢[ 3 ]。在大鼠肝脏和心脏线粒体中，UK-5099抑制丙酮酸盐依赖型02的消耗，IC50值为50 nM [4]。
参考文献：
[1]. Wiemer EA, Michels PA, Opperdoes FR. The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications. Biochem J, 1995, 312 ( Pt 2): 479-484.
[2]. Halestrap AP. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J, 1975, 148(1): 85-96.
[3]. Halestrap AP, Armston AE. A re-evaluation of the role of mitochondrial pyruvate transport in the hormonal control of rat liver mitochondrial pyruvate metabolism. Biochem J, 1984, 223(3): 677-685.
[4]. Proudlove MO, Beechey RB, Moore AL. Pyruvate transport by thermogenic-tissue mitochondria. Biochem J, 1987, 247(2): 441-447.
| Cell experiment:[1] | |
Cell lines | 832/13 cells derived from INS-1 rat insulinoma cells |
Reaction Conditions | 50 ~ 150 μM UK-5099 for 30 ~ 65 min incubation |
Applications | UK-5099 significantly inhibited the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. Moreover, UK-5099 (150 μM) reduced ATP levels and increased ADP and AMP levels in 832/13 cells. |
| Animal experiment:[1] | |
Animal models | C57BLK mice |
Dosage form | 32 μmol/kg Injected intraperitoneally 30 min before the glucose challenge |
Applications | UK-5099 caused a significantly greater glucose excursion at 30, 60, and 120 min as compared with DMSO control mice. The area under the curve was also significantly increased by UK-5099 as compared with DMSO control mice. Thus, UK-5099 resulted in impaired glucose tolerancein vivo. |
Note | The technical data provided above is for reference only. |
References: 1. Patterson JN, Cousteils K, Lou JW, et al Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated insulin secretion. Journal of Biological Chemistry, 2014, 289(19): 13335-13346. | |
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