1. Metabolic Enzyme/Protease
  2. Mitochondrial Metabolism
  3. GW604714X

GW604714X 

目录号: HY-138559
产品使用指南

GW604714X 是丙酮酸支持的线粒体呼吸 (mitochondrial respiration) 的有效选择性抑制剂。GW604714X 抑制线粒体丙酮酸载体 (MPC) 的 Ki 值 <0.1 μM。GW604714X 也能抑制质膜单羧酸转运蛋白 MCT1 对 L-乳酸的转运,但其浓度要比 MPC 高 4 个数量级。

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GW604714X Chemical Structure

GW604714X Chemical Structure

CAS No. : 853953-65-8

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Description

GW604714X is a potent and selective inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X inhibits the mitochondrial pyruvate carrier (MPC) with a Ki values <0.1 μM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter MCT1, but at concentrations more than four orders of magnitude greater than the MPC[1].

In Vitro

GW604714X inhibits the mitochondrial pyruvate carrier (MPC) with Ki values <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[1].
GW604714X inhibits the transport of 0.5 mM [14C]-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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

471.46

Formula

C₂₁H₁₈FN₅O₅S

CAS No.

853953-65-8

SMILES

O=C(NC/1=O)SC1=C/C2=CC(C3=NC(N4CCN(C(C)=O)CC4)=CC=C3[N+]([O-])=O)=CC=C2F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

GW604714XMitochondrial Metabolismmitochondrial respirationMPCMCT1pyruvateInhibitorinhibitorinhibit

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产品名称:
GW604714X
目录号:
HY-138559
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