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AZD7545

Catalog No. T2447Cas No. 252017-04-2

AZD7545 is a potent PDHK inhibitor.

AZD7545

AZD7545

Purity: 99.13%
Catalog No. T2447Cas No. 252017-04-2
AZD7545 is a potent PDHK inhibitor.
Pack SizePriceAvailabilityQuantity
1 mg$40In Stock
5 mg$92In Stock
10 mg$139In Stock
25 mg$239In Stock
50 mg$372In Stock
100 mg$513In Stock
1 mL x 10 mM (in DMSO)$97In Stock
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Purity:99.13%
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Product Introduction

Bioactivity
Description
AZD7545 is a potent PDHK inhibitor.
Targets&IC50
PDHK2:6.4 nM, PDHK1:36.8 nM
In vitro
In obese, insulin-resistant Zucker rats, AZD7545 eliminated postprandial hyperglycemia. AZD7545 increased the percentage of active PDH in the liver and skeletal muscle of Wistar rats.
In vivo
AZD7545 inhibits pyruvate dehydrogenase kinase (PDHK) activity by disrupting the interaction between the inner lipoic acid domain of PDHK2 and the dihydrolipoamide acetyltransferase component of the pyruvate dehydrogenase complex (PDC). It increases the activity of pyruvate dehydrogenase (PDH) in primary rat hepatocytes with an EC50 of 105 nM. In the presence of recombinant human PDHK2, AZD7545 also enhances PDH activity, achieving an EC50 of 5.2 nM.
Kinase Assay
Cellular Kinase Assays: NIH3T3 cells prepared by transfection of human KDR. The cells are cultured in a collagen type I coated 96-well plate in an amount of 1.5 × 104 per well. The medium is then replaced by a DMEM medium containing 0.1% FCS. Ki8751 diluted in DMSO is added to each well and cultured. rhVEGF is added to a final concentration of 100 ng/mL, and the stimulation of cells is carried out at 37 °C. The cells are washed with PBS (pH 7.4), 50 μL of a solubilization buffer (20 mM HEPES (pH 7.4), 150 mM NaCl, 0.2% Triton X-100, 10% glycerol, 5 mM Na3VO4, 5 mM disodium ethylenediamine tetraacetate, and 2 mM Na4P2O7) is then added and a cell extract is prepared. Separately, PBS (50 μL, pH 7.4) containing 5 μg/mL of antiphosphotyrosine antibody (PY20) is added to a microplate for ELISA. After washing of the plate, 300 μL of a blocking solution is added. The cell extract is transferred to the plate. An anti-VEGFR2 antibody and a peroxidase-labeled anti-rabbit Ig antibody are added. Next, a chromophoric substrate for peroxidase is added, and the absorbance at 450 nm is measured with microplate reader. The VEGFR2 phosphorylation activity for each well is determined by presuming the absorbance with the addition of VEGF and without the addition of the test sample to be 100% VEGFR2 phosphorylation activity and VEGF to be 0% VEGFR2 phosphorylation activity. The concentration of the inhibition (%) of VEGFR2 Phosphorylation is determined for each case, and IC50 value is calculated.
Chemical Properties
Molecular Weight478.87
FormulaC19H18ClF3N2O5S
Cas No.252017-04-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 88 mg/mL (183.8 mM)
DMSO: 88 mg/mL (183.8 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.0882 mL10.4412 mL20.8825 mL104.4125 mL
5 mM0.4176 mL2.0882 mL4.1765 mL20.8825 mL
10 mM0.2088 mL1.0441 mL2.0882 mL10.4412 mL
20 mM0.1044 mL0.5221 mL1.0441 mL5.2206 mL
50 mM0.0418 mL0.2088 mL0.4176 mL2.0882 mL
100 mM0.0209 mL0.1044 mL0.2088 mL1.0441 mL

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