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UK-5099

 
Catalog No.
A3899
MCTs和MPC抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 909.00
现货
50mg
¥ 3,090.00
现货

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A

背景

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.

文献引用

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt288.3
Cas No.56396-35-1
FormulaC18H12N2O2
SynonymsPF-1005023;UK5099;UK 5099;PF1005023;PF 1005023
Solubilityinsoluble 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
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O
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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 tolerance in 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.

质量控制

化学结构

UK-5099

相关生物数据

UK-5099