PF-249

PF-249 is an allosteric activator of AMP-activated protein kinase beta1 (AMPKbeta1) heterotrimers (EC50s = 8 and 6 nM for human AMPK alpha1beta1gamma1 and -alpha2beta1gamma1, respectively). It is selective for AMPK alpha1beta1gamma1 and -alpha2beta1gamma1 over AMPK alpha1beta2gamma1, -alpha2beta2gamma1, and -alpha2beta2gamma3 at 40 µM and a panel of receptors, channels, and phosphodiesterases at 10 µM. PF-249 decreases proteinuria and improves kidney function in an obese ZSF1 rat model of diabetic nephropathy in a dose-dependent manner.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: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 1 mg/ml, Ethanol: 5 mg/ml. lambdamax: 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.