pf-249

Description: PF-249, formerly known as PF-06685249, is a beta1-selective AMPK agonist. PF-06685249 is a potent AMPK activator. PF-06685249 exhibited robust activation of AMPK in rat kidneys as well as desirable orally bioavailable absorption, low plasma clearance, and negligible renal clearance in preclinical species.

References: Cokorinos EC, Delmore J, Reyes AR, Albuquerque B, Kjøbsted R, Jørgensen NO, Tran JL, Jatkar A, Cialdea K, Esquejo RM, Meissen J, Calabrese MF, Cordes J, Moccia R, Tess D, Salatto CT, Coskran TM, Opsahl AC, Flynn D, Blatnik M, Li W, Kindt E, Foretz M, Viollet B, Ward J, Kurumbail RG, Kalgutkar AS, Wojtaszewski JFP, Cameron KO, Miller RA. Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice. Cell Metab. 2017 May 2; 25(5):1147-1159.e10. doi: 10.1016/j.cmet.2017.04.010. PubMed PMID: 28467931.