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PF-06409577

CAS No. : 1467057-23-3

MCE 站：PF-06409577

产品活性：PF-06409577是有效，选择性的AMPK α1β1γ1 亚型变构激活剂，EC₅₀ 值为7 nM。

研究领域：Epigenetics  |  PI3K/Akt/mTOR

作用靶点：AMPK

In Vitro: PF-06409577 possesses similar potency toward the human and rat α1β1γ1 isoforms. In broad panel screening against other receptors, channels, PDEs and kinases, PF-06409577 exhibits minimal off-target pharmacology. PF-06409577 shows no detectable inhibition of hERG in a patch-clamp assay (100 ?M) and is not an inhibitor (IC₅₀>100 ?M) of the microsomal activities of major human cytochrome P450 isoforms.

In Vivo: PF-06409577 demonstrates moderate plasma clearance in rats, dogs, and monkeys, and is well distributed with steady state distribution volume. Following oral administration of crystalline PF-06409577 in 0.5% methylcellulose suspension, PF-06409577 is rapidly absorbed in rats, dogs, and monkeys. The corresponding oral bioavailability values in rats, dogs, and monkeys, are 15%, 100%, and 59%, respectively. Dose responsive increases in pAMPK relative to total AMPK (tAMPK) in whole kidney tissue are observed with a maximal 3.8-fold response at 300 mg/kg PF-06409577 treatment. Oral administration of PF-06409577 (10, 30, and 100 mg/kg QD) results in dose-dependent reductions in proteinuria in the obese ZSF1 animals, with greater than 2-fold reduction in 24-hour urinary albumin loss compared to vehicle control after 60 days of treatment.

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