UK-5099

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UK-5099

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

56396-35-1

包装与价格：

包装	价格(元)
10mg	询价
50mg	询价

化学性质

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。

资料参考

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.

试验操作

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.