An allosteric activator of AMPKβ1 heterotrimers
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PF-249

Item No. 38416

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-5-[6-(dimethylamino)-2-methoxy-3-pyridinyl]-1H-indole-3-carboxylic acid
CAS Number
1467059-70-6
Synonyms
  • PF-06885249
Molecular Formula
C17H16ClN3O3
Formula Weight
345.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 1 mg/mlEthanol: 5 mg/ml
λmax
224, 255, 301 nm
SMILES
O=C(C1=CNC2=C1C=C(C3=C(OC)N=C(N(C)C)C=C3)C(Cl)=C2)O
InChi Code
InChI=1S/C17H16ClN3O3/c1-21(2)15-5-4-9(16(20-15)24-3)10-6-11-12(17(22)23)8-19-14(11)7-13(10)18/h4-8,19H,1-3H3,(H,22,23)
InChi Key
MJHBRTGGZYSCHJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $40

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    5 mg

    $179

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    10 mg

    $315

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    25 mg

    $590

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    Product Description

    PF-249 is an allosteric activator of AMP-activated protein kinase β1 (AMPKβ1) heterotrimers (EC50s = 8 and 6 nM for human AMPK α1β1γ1 and -α2β1γ1, respectively).1,2 It is selective for AMPK α1β1γ1 and -α2β1γ1 over AMPK α1β2γ1, -α2β2γ1, and -α2β2γ3 at 40 µM and a panel of receptors, channels, and phosphodiesterases at 10 µM.1,2 PF-249 decreases proteinuria and improves kidney function in an obese ZSF1 rat model of diabetic nephropathy in a dose-dependent manner.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Salatto, C.T., Miller, R.A., Cameron, K.O., et al. Selective activation of AMPK β1-containing isoforms improves kidney function in a rat model of diabetic nephropathy. J. Pharmacol. Exp. Ther. 361(2), 303-311 (2017).

    2. Ryder, T.F., Calabrese, M.F., Walker, G.S., et al. Acyl glucuronide metabolites of 6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid (PF-06409577) and related indole-3-carboxylic acid derivatives are direct activators of adenosine monophosphate-activated protein kinase (AMPK). J. Med. Chem. 61(16), 7273-7288 (2018).