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

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 Ki <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.

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GW604714X Chemical Structure

GW604714X Chemical Structure

CAS No. : 853953-65-8

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Based on 1 publication(s) in Google Scholar

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Description

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 Ki <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[1].

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[1].
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].

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

Molecular Weight

471.46

Formula

C21H18FN5O5S

CAS No.
Appearance

Solid

Color

Light yellow to green yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMF : 5.26 mg/mL (11.16 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1211 mL 10.6054 mL 21.2107 mL
5 mM 0.4242 mL 2.1211 mL 4.2421 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
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Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMF 1 mM 2.1211 mL 10.6054 mL 21.2107 mL 53.0268 mL
5 mM 0.4242 mL 2.1211 mL 4.2421 mL 10.6054 mL
10 mM 0.2121 mL 1.0605 mL 2.1211 mL 5.3027 mL
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GW604714X Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GW604714X
Cat. No.:
HY-138559
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