An AMPK activator
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PF-06409577

Item No. 27366

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid
CAS Number
1467057-23-3
Molecular Formula
C19H16ClNO3
Formula Weight
341.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
245, 289 nm
SMILES
ClC(C=C(NC=C1C(O)=O)C1=C2)=C2C3=CC=C(C4(O)CCC4)C=C3
InChi Code
InChI=1S/C19H16ClNO3/c20-16-9-17-14(15(10-21-17)18(22)23)8-13(16)11-2-4-12(5-3-11)19(24)6-1-7-19/h2-5,8-10,21,24H,1,6-7H2,(H,22,23)
InChi Key
FHQXLWCFSUSXBF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $186

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    25 mg

    $378

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for α1β1γ1).1 In vitro, it selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM). PF-06409577 has an EC50 value of 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK. In vivo, PF-06409577 (≥10 mg/kg) increases phosphorylation of AMPK in rat kidney. It decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease when administered at a dose of 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cameron, K.O., Kung, D.W., Kalgutkar, A.S., et al. Discovery and preclinical characterization of 6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid (PF-06409577), a direct activator of adenosine monophosphate-activated protein kinase (AMPK), for the potential treatment of diabetic nephropathy. J. Med. Chem. 59(17), 8068-8081 (2016).