Name: PF-05175157
Brand: Selleck Chemicals
SKU: S6672
Availability: InStock
Rating: 5 (3 reviews)

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Quality Control

Batch: Purity: 99.85%

99.85

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Acetyl-CoA carboxylase Inhibitors	Firsocostat (GS-0976, ND-630) CP 640186 ND646 TOFA 4-Methylsalicylic acid PF-05221304 Oxalacetic acid

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (73.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (3.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.750mg/ml (1.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight

405.49

Formula

C₂₃H₂₇N₅O₂

Storage (From the date of receipt)

3 years -20°C powder

CAS No.

1301214-47-0

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Storage of Stock Solutions

1 year-80°Cin solvent
1 month-20°Cin solvent

Synonyms

N/A

Smiles

CC1=NC2=C(N1)C=C(C=C2)C(=O)N3CCC4(CC3)CC5=C(C(=O)C4)N(N=C5)C(C)C

Mechanism of Action

Targets/IC₅₀/Ki	rACC1 (Cell-free assay) 23.5 nM hACC1 (Cell-free assay) 27.0 nM hACC2 (Cell-free assay) 33.0 nM rACC2 (Cell-free assay) 50.4 nM
In vitro	The in vitro metabolism of PF-05175157 is evaluated in microsomes from rat, dog, and human hepatocytes. This compound is not metabolized in rat, dog, or human microsomes. It 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. This chemical 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	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 this compound, 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25423286-decreasing-the-rate-of-metabolic-ketone-reduction-in-the-discovery-of-a-clinical-acetyl-coa-carboxylase-inhibitor-for-the-treatment-of-diabetes/?from_single_result=Decreasing+the+Rate+of+Metabolic+Ketone+Reduction+in+the+Discovery+of+a+Clinical+Acetyl-CoA+Carboxylase+Inhibitor+for+the+Treatment+of+Diabetes

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02100527	Withdrawn	Acne Vulgaris	Pfizer	April 2014	Phase 2
NCT02053116	Terminated	Type 2 Diabetes Mellitus	Pfizer	March 2014	Phase 2
NCT02053103	Terminated	Type 2 Diabetes Mellitus	Pfizer	March 2014	Phase 2
NCT01807377	Completed	Diabetes Mellitus Type 2	Pfizer	April 2013	Phase 1
NCT01792635	Terminated	Diabetes Mellitus Type 2	Pfizer	December 2012	Phase 2
NCT01537497	Completed	Diabetes Mellitus Type 2	Pfizer	March 2012	Phase 1

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PF-05175157 Acetyl-CoA carboxylase inhibitor

Chemical Structure

Molecular Weight: 405.49