PF-05175157

Biological Activity

In vitro: 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.

Product Citations

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  Patent. CN118652982B 2025 Jun 24; .

  Patent. CN118652982B
  PF-05175157 purchased from AbMole

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  Patent. CN118652982A 2024 Sep 17.

  Patent. CN118652982A
  PF-05175157 purchased from AbMole

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  Patent. CN118792406A 2024 Oct 18.

  Patent. CN118792406A
  PF-05175157 purchased from AbMole

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  Drug Dev Res. 2023 Aug 11.

  FAM64A aggravates proliferation, invasion, lipid droplet formation, and chemoresistance in gastric cancer: A biomarker for aggressiveness and a gene therapy target
  PF-05175157 purchased from AbMole

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  World J Gastroenterol. 2023 Sep 21;29(35): 5104-5124.

  Regenerating gene 4 promotes chemoresistance of colorectal cancer by affecting lipid droplet synthesis and assembly
  PF-05175157 purchased from AbMole

Protocol (for reference only)

Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time

Animal Experiment
Animal models	Male SD rats
Formulation	0.5% methyl cellulose: 0.1% polysorbate 80
Dosages	0.25, 0.5, 1, 2, 4, 8, 15, 25, 50, and 100 mg/kg
Administration	oral

Chemical Information

Molecular Weight	405.49
Formula	C23H27N5O2
CAS Number	1301214-47-0
Solubility (25°C)	DMSO 30 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month