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Cat. No. M6137

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PF-05175157 Structure


Size Price Availability Quantity
10mM*1mL in DMSO USD 72  USD72 In stock
1mg USD 30  USD30 In stock
5mg USD 72  USD72 In stock
10mg USD 121  USD121 In stock
25mg USD 240  USD240 In stock
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Quality Control & Documentation
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
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
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

[1] Griffith DA, et al. J Med Chem. Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes.

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Abmole Inhibitor Catalog

Keywords: PF-05175157, PF05175157 supplier, Acetyl-CoA Carboxylase, inhibitors, activators

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