A PDK inhibitor
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AZD 7545

Item No. 19282

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethyl-benzamide
CAS Number
252017-04-2
Molecular Formula
C19H18ClF3N2O5S
Formula Weight
478.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mLDMSO: 50 mg/mLDMSO:PBS(pH 7.2): 0.02 mg/mLEthanol: 20 mg/mL
λmax
208, 273 nm
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
InChi Code
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)
InChi Key
DTDZLJHKVNTQGZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

    $161

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    10 mg

    $302

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    25 mg

    $696

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    AZD 7545 is an inhibitor of pyruvate dehydrogenase (PDH) kinases (PDKs), resulting in an increase in PDH activity with an EC50 value of 5.2 nM for PDK2.1,2 It less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).3 AZD 7545 stimulates pyruvate oxidation in rat hepatocytes (EC50 = 105 nM) and significantly elevates muscle PDH activity in obese Zucker rats.1 It elevates postprandial glucose levels and improves the 24 hour glucose profile in obese, insulin-resistant rats, compared with lean counterparts.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mayers, R.M., Butlin, R.J., Kilgour, E., et al. 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. Biochem. Soc. Trans. 31(Pt 6), 1165-1167 (2003).

    2. Morrell, J.A., Orme, J., Roche, T.E., et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem. Soc. Trans. 31(Pt 6), 1168-1170 (2016).

    3. Kato, M., Li, J., Chuang, J.L., et al. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol. Structure 15(8), 992-1004 (2007).