GW604714X
目录号: PL07313 纯度: ≥98%
CAS No. :853953-65-8
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中文名称
GW604714X
英文名称
GW604714X
英文别名
5-(5-(6-(4-Acetylpiperazin-1-yl)-3-nitropyridin-2-yl)-2-fluorobenzylidene)thiazolidine-2,4-dione;(5Z)-5-[[5-[6-(4-Acetylpiperazin-1-yl)-3-nitropyridin-2-yl]-2-fluorophenyl]methylidene]-1,3-thiazoli;GW604714X
Cas No.
853953-65-8
分子式
C21H18FN5O5S
分子量
471.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GW604714X 是一种有效的线粒体呼吸 (mitochondrial respiration) 抑制剂。GW604714X 是一种高度特异性的线粒体丙酮酸载体 (MPC) 抑制剂,Ki <0.1 nM。GW604714X 也能抑制质膜单羧酸转运体 (MCT1) 的 L-乳酸转运,但浓度比 MPC 的大 4 个数量级。
生物活性
GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a K i <0.1 nM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC.
性状
Solid
体外研究(In Vitro)
GW604714X inhibits the mitochondrial pyruvate carrier (MPC) with Ki value <0.1 μM in direct measurement of pyruvate transport into rat liver and yeast mitochondria.
Inhibitor titrations of pyruvate-dependent respiration by heart mitochondria gave values for the concentration of inhibitor binding sites and their Ki (nM) of 56.0 nM and 0.057 nM for the GW604714X.
GW604714X inhibits the transport of 0.5 mM [C]-l-lactate into rat red blood cells, mediated by the monocarboxylate transporter MCT1. GW604714X at 10 μM reduces the initial rate of uptake to 30% of control values.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. John C W Hildyard, et al. Identification and characterisation of a new class of highly specific and potent inhibitors of the mitochondrial pyruvate carrier. Biochim Biophys Acta. Apr-May 2005;1707(2-3):221-30.
[2]. Allen K. Bourdon, et al. Alzheimers and Parkinsons Disease Novel Therapeutic Target: The Mitochondrial Pyruvate Carrier - Ligand Docking to Screen Natural Compounds Related to Classic Inhibitors. DOI:10.4018/IJKDB.2017070104
溶解度数据
In Vitro: DMF : 5.26 mg/mL (11.16 mM; Need ultrasonic and warming)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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