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PF-05175157

CAS No. : 1301214-47-0

MCE 国际站：PF-05175157

产品活性：PF-05175157 是一种广谱乙酰辅酶 A 羧化酶 (ACC) 抑制剂，对 ACC1 (human)，ACC2 (human)， ACC1 (rat) 和 ACC2 (rat) 的 IC₅₀ 值分别为 27.0, 33.0, 23.5 和 50.4 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acetyl-CoA Carboxylase

In Vitro: PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀s of 27.0±2.7, 33.0±4.1, 23.5±1.1 and 50.4±2.6 nM for ACC1 (human), ACC2 (human), ACC1 (rat) and ACC2 (rat), respectively. The in vitro metabolism of PF-05175157 (Compound 9) is evaluated in microsomes from rat, dog, and human hepatocytes. PF-05175157 is not metabolized in rat, dog, or human microsomes. PF-05175157 is also stable in human hepatocyte incubations, but is minimally metabolized by recombinant human CYP3A4 and CYP3A5. PF-05175157 inhibits formation of malonyl-CoA in a concentration-dependent manner with a potency (EC₅₀=30 nM) in rat hepatocytes consistent with its potency against rat ACC1 (24 nM).

In Vivo: Oral administration (3 mg/kg) to rats and dogs show bioavailability of 40% and 54%, respectively, consistent with the low microsomal clearance and good solubility at low pH. Formation of the direct product of ACC, malonyl-CoA, in the skeletal muscle and liver of lean rats is assessed 1 h following an acute oral dose of PF-05175157, showing concentration-dependent reductions in both skeletal muscle and liver malonyl-CoA. At the nadir, quadriceps and liver malonyl-CoA levels are reduced by 76% and 89%, respectively. The EC₅₀s for inhibition of quadriceps and liver malonyl-CoA are 870 and 540 nM, respectively, determined from unbind plasma concentrations of PF-05175157. Acute oral administration of PF-05175157 inhibits hepatic DNL in rats in an unbind plasma drug concentration-dependent manner. PF-05175157 inhibits up to 82% of the incorporation of [¹⁴C]acetate into [¹⁴C]lipids with an EC₅₀ of 326 nM.

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