PF-05175157

For research use only.

Catalog No.S6672

PF-05175157 Chemical Structure

Molecular Weight(MW): 405.49

PF-05175157 is a broad-spectrum effective ACC inhibitor with IC50 of 27.0 nM, 33.0 nM, 23.5 nM and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively.

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USD 277 In stock
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Purity & Quality Control

Choose Selective Acetyl-CoA carboxylase Inhibitors

Biological Activity

Description PF-05175157 is a broad-spectrum effective ACC inhibitor with IC50 of 27.0 nM, 33.0 nM, 23.5 nM and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively.
Targets
rACC1 [1]
(Cell-free assay)
hACC1 [1]
(Cell-free assay)
hACC2 [1]
(Cell-free assay)
rACC2 [1]
(Cell-free assay)
23.5 nM 27.0 nM 33.0 nM 50.4 nM
In vitro

The in vitro metabolism of PF-05175157 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, suggesting it is a substrate for 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).[1]

In vivo

In vivo, the plasma clearance of PF-05175157 is low following intravenous (iv) administration (1 mg/kg) to rats, dogs, and monkeys. Oral (po) administration (3 mg/kg) to rats and dogs showed bioavailability of 40% and 54%, respectively, consistent with the low microsomal clearance and good solubility at low pH. The bioavailability following a 50 mg/kg oral dose in rats was 106%, suggesting saturation of clearance. Formation of the direct product of ACC, malonyl-CoA, in the skeletal muscle and liver of lean Sprague Dawley 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. [1]

Protocol

Cell Research:

[1]

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  • Cell lines: rat hepatocytes
  • Concentrations: --
  • Incubation Time: 5 h
  • Method:

    On the day of the study, media was aspirated and cells are treated with fresh MCM media containing DMSO vehicle or varying concentrations of PF-05175157 as indicated. Compound was initially dissolved in DMSO and subsequently diluted 1:100 in MCM.After 5 h at 37 °C, incubation media is removed and the experiment is terminated by washing the cells with ice cold PBS.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male SD rats
  • Dosages: 0.25mg/kg, 0.5mg/kg, 1mg/kg, 2mg/kg, 4mg/kg, 8mg/kg, 15mg/kg, 25mg/kg, 50mg/kg and 100 mg/kg
  • Administration: Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 30 mg/mL (73.98 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 405.49
Formula

C23H27N5O2

 

CAS No. 1301214-47-0
Storage powder
in solvent
Synonyms N/A

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02100527 Withdrawn Drug: PF-05175157|Drug: Placebo Acne Vulgaris Pfizer April 2014 Phase 2
NCT02053116 Terminated Drug: PF-05175157|Drug: Placebo Type 2 Diabetes Mellitus Pfizer March 2014 Phase 2
NCT02053103 Terminated Drug: PF-05175157|Drug: Placebo Type 2 Diabetes Mellitus Pfizer March 2014 Phase 2
NCT01807377 Completed Drug: PF-05175157|Drug: Midazolam|Other: Placebo Diabetes Mellitus Type 2 Pfizer April 2013 Phase 1
NCT01792635 Terminated Drug: PF-05175157|Drug: Placebo Diabetes Mellitus Type 2 Pfizer December 2012 Phase 2
NCT01537497 Completed Drug: PF-05175157|Drug: Placebo Diabetes Mellitus Type 2 Pfizer March 2012 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID