MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

PF-05175157

CAS No. : 1301214-47-0

MCE 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  TOFA  |  Fluazifop-P-butyl  |  Propaquizafop

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。