PF-06409577

PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for alpha1beta1gamma1). In vitro, it selectively activates beta1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over beta2-containing isoforms (EC50s = >10 µM). PF-06409577 has an EC50 value of 7 nM in an activation/protection TR-FRET assay using alpha1beta1gamma1 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.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: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 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.