AdipoGen Life Sciences

AZD 7545

CHF 50.00

In stock

AG-CR1-3692-M0011 mgCHF 50.00

AG-CR1-3692-M0055 mgCHF 160.00

AG-CR1-3692-M01010 mgCHF 290.00

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Product Details
Synonyms	4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethyl-benzamide
Product Type	Chemical
Properties
Formula	C₁₉H₁₈ClF₃N₂O₅S
MW	478.9
CAS	252017-04-2
Purity Chemicals	≥98% (HPLC)
Appearance	White to off-white solid.
Solubility	Soluble in DMSO (40mg/ml), ethanol (20mg/ml) or DMF (20mg/ml).
Identity	Determined by ¹H-NMR
InChi Key	DTDZLJHKVNTQGZ-UHFFFAOYSA-N
Smiles	O=C(N(C)C)C1=CC=C(S(C2=CC(Cl)=C(NC([C@](O)(C)C(F)(F)F)=O)C=C2)(=O)=O)C=C1
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry. Protect from light.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Description

Potent and selective pyruvate dehydrogenase kinase 2 (PDK2) inhibitor (IC₅₀=6.4nM), consequently increasing pyruvate dehydrogenase (PDH) activity. Less potent inhibitor towards PDK1 and PDK3 (IC₅₀=87 and 600nM, respectively).
Inhibitor of glycolysis.
Antiobesity and antidiabetic agent. Improves blood glucose control in obese (fa/fa) Zucker rats.
Useful agent for immunometabolism research.
To maintain a continuous and steady supply of ATP during the feed-fast cycle, cells must select fatty acid or glucose for fuel. This process is largely controlled by the pyruvate dehydrogenase complex (PDC), which regulates the entry of glycolytic products into the tricarboxylic acid cycle by catalyzing the oxidative decarboxylation of pyruvate to acetyl-coenzyme A (CoA) in the mitochondria of mammalian cells. PDKs and pyruvate dehydrogenase phosphatases (PDPs) are key regulators of PDC activity, and they act in a phosphorylation-dephosphorylation manner.

Product References

AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats: R.M. Mayers, et al.; Biochem. Soc. Trans. 31, 1165 (2003)
AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2: J.A. Morrell, et al.; Biochem. Soc. Trans. 31, 1168 (2003)
Recognition of the inner lipoyl-bearing domain of dihydrolipoyl transacetylase and of the blood glucose-lowering compound AZD7545 by pyruvate dehydrogenase kinase 2: A. Tuganova, et al.; Biochem. 46, 8592 (2007)
Distinct Structural Mechanisms for Inhibition of Pyruvate Dehydrogenase Kinase Isoforms by AZD7545, Dichloroacetate, and Radicicol: M. Kato, et al.; Cell Structure 15, 992 (2007)
Dichloroacetate induces regulatory T-cell differentiation and suppresses Th17-cell differentiation by pyruvate dehydrogenase kinase-independent mechanism: N. Makita, et al.; J. Pharm. Pharmacol. 69, 43 (2017)

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