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GW604714X

GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) 是一种高度特异性的线粒体丙酮酸载体抑制剂，Ki<0.1 nM。它是一种线粒体呼吸抑制剂。它也能抑制质膜单羧酸转运体的 L-乳酸转运，但浓度比 MPC 的大 4 个数量级。

CAS号

853953-65-8

分子式

C21H18FN5O5S

主要靶点

Mitochondrial Metabolism

仅限科研使用

Cat No : CM05203

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Synonyms

2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-

验证数据展示

  • CAS No.: 853953-65-8

    GW604714X
    CAS#: 853953-65-8

产品信息

GW604714X were found to be potent inhibitors of mitochondrial respiration supported by pyruvate

CAS号 853953-65-8
分子式 C21H18FN5O5S
主要靶点 Mitochondrial Metabolism
主要通路 代谢
分子量 471.46
纯度 99.03%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-

体外活性

Direct measurement of pyruvate transport into rat liver and yeast mitochondria confirmed that these agents inhibited the mitochondrial pyruvate carrier (MPC) with K(i) values <0.1 μM. Inhibitor titrations of pyruvate-dependent respiration by heart mitochondria gave values for the concentration of inhibitor binding sites (pmol per mg protein) and their K(i) (nM) of 56.0 and 0.057 nM for the more hydrophobic GW604714X. GW604714X inhibited l-lactate transport by the plasma membrane monocarboxylate transporter MCT1, but at concentrations more than four orders of magnitude greater than the MPC.

溶解度

DMF:5mg/ml(10.61mM),Sonification is recommended.,DMSO:4 mg/mL (8.48 mM)

参考文献

1.Hildyard J , Mml C , Dukes I D , et al. Identification and characterisation of a new class of highly specific and potent inhibitors of the mitochondrial pyruvate carrier[J]. Biochimica et Biophysica Acta (BBA) - Bioenergetics, 2005, 1707(2-3):221-230.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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