AZD 7545
| Code | Size | Price |
|---|
| AG-CR1-3692-M001 | 1 mg | £45.00 |
Quantity:
| AG-CR1-3692-M005 | 5 mg | £140.00 |
Quantity:
| AG-CR1-3692-M010 | 10 mg | £250.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Target Species: Universal
Shipping:
AMBIENT
Storage:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethyl-benzamide
Appearance:
White to off-white solid.
CAS:
252017-04-2
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.Protect from light.
InChi:
InChI=1S/C19H18ClF3N2O5S/c1-18(28,19(21,22)23)17(27)24-15-9-8-13(10-14(15)20)31(29,30)12-6-4-11(5-7-12)16(26)25(2)3/h4-10,28H,1-3H3,(H,24,27)
InChiKey:
DTDZLJHKVNTQGZ-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 252017-04-2. Formula: C19H18ClF3N2O5S. MW: 478.9. . 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.
MDL:
MFCD25976792
Molecular Formula:
C19H18ClF3N2O5S
Molecular Weight:
478.9
Package Type:
Vial
Product 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.
Purity:
>98% (HPLC)
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
Solubility Chemicals:
Soluble in DMSO (40mg/ml), ethanol (20mg/ml) or DMF (20mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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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