GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Information
AZD7545 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 ; PDHK1 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. 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.
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.
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.
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
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Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of pyruvate dehydrogenase kinase 1;Inhibitor of pyruvate dehydrogenase kinase 2
This compound belongs to the class of organic compounds known as benzamides. These are organic compounds containing a carboxamido substituent attached to a benzene ring.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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