AZD7545

Catalog No.S7517 Batch:S751701

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Technical Data

Formula

C19H18ClF3N2O5S
Molecular Weight 478.87 CAS No. 252017-04-2
Solubility (25°C)* In vitro DMSO 95 mg/mL (198.38 mM)
Ethanol 95 mg/mL (198.38 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.79mg/ml Taking the 1 mL working solution as an example, add 50 μL of 15.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.75mg/ml Taking the 1 mL working solution as an example, add 50 μL of 95 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description AZD7545 is a potent PDHK inhibitor with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. It failed to inhibit PDHK4 at higher concentrations(>10 nM), AZD7545 stimulates PDHK4 activity.
Targets
PDHK2 [1] PDHK1 [1]
6.4 nM 36.8 nM
In vitro In the presence of recombinant human PDHK2, AZD7545 increases PDH activity with EC50 of 5.2 nM. In primary rat hepatocytes, AZD7545 increases PDH activity with EC50 of 105 nM. [2] AZD7545 inhibits PDHK activity by disrupting the interactions between PDHK2 and the inner lipoyl-bearing domains (L2) of the dihydrolipoyl transacetylase component (E2) of PDC. [3]
In vivo In Wistar rats, AZD7545 increases the percentage of active PDH in the liver and skeletal muscle. In obese, insulin-resistant, Zucker rats, AZD7545 eliminates the postprandial elevation in blood glucose. [2]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Mol Cancer, 2017, 16(1):102]

Data from [Data independently produced by , , J Pharm Pharmacol, 2017, 69(1):43-51]

Selleck's AZD7545 has been cited by 11 publications

Hypoxia-induced reprogramming of glucose-dependent metabolic pathways maintains the stemness of human bone marrow-derived endothelial progenitor cells [ Sci Rep, 2023, 13(1):8776] PubMed: 37258701
Systemic Metabolic and Mitochondrial Defects in Rett Syndrome Models [ bioRxiv, 2023, 10.1101/2023.04.03.535431] PubMed: None
Systemic Metabolic and Mitochondrial Defects in Rett Syndrome Models [ bioRxiv, 2023, 2023.04.03.535431] PubMed: 37066332
Inhibition of aberrant Hif1α activation delays intervertebral disc degeneration in adult mice [ Bone Res, 2022, 10(1):2] PubMed: 34983922
The Combined Use of Orf Virus and PAK4 Inhibitor Exerts Anti-tumor Effect in Breast Cancer [ Int J Mol Sci, 2022, 23(7)3745] PubMed: 35409102
Increased demand for NAD+ relative to ATP drives aerobic glycolysis [ Mol Cell, 2021, 81(4):691-707.e6] PubMed: 33382985
mTOR-mediated cancer drug resistance suppresses autophagy and generates a druggable metabolic vulnerability [ Nat Commun, 2020, 11(1):4684] PubMed: 32943635
Increased demand for NAD+ relative to ATP drives aerobic glycolysis [ Mol Cell, 2020, S1097-2765(20)30904-7] PubMed: 33382985
ROS production induced by BRAF inhibitor treatment rewires metabolic processes affecting cell growth of melanoma cells. [Cesi G, et al. Mol Cancer, 2017, 16(1):102] PubMed: 28595656
Dichloroacetate induces regulatory T-cell differentiation and suppresses Th17-cell differentiation by pyruvate dehydrogenase kinase-independent mechanism [ J Pharm Pharmacol, 2017, 69(1):43-51] PubMed: 27757958

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.