PF-04620110

Catalog No.S7192

For research use only.

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

PF-04620110 Chemical Structure

CAS No. 1109276-89-2

Selleck's PF-04620110 has been cited by 2 Publications

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
Targets
DGAT1 [1]
19 nM
In vivo In Rats, PF-04620110 reduces plasma triglyceride levels t doses of ≥0.1 mg/kg following a lipid challenge. [1] DGAT1 inhibition by PF-04620110 causes an enrichment of polyunsaturated fatty acids within the TG class of lipids in rodents. [2]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Male Sprague Dawley rats
  • Dosages: ~10 mg/kg
  • Administration: p.o.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 49 mg/mL warmed
(123.6 mM)
Water Insoluble
Ethanol Insoluble

* 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 396.44
Formula

C21H24N4O4

CAS No. 1109276-89-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)N3CCOC4=NC=NC(=C4C3=O)N

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01298518 Completed Drug: PF-04620110|Drug: Placebo Type 2 Diabetes Patients Pfizer February 2011 Phase 1
NCT01166217 Completed Drug: PF-04620110 Healthy Pfizer|Bristol-Myers Squibb July 2010 Phase 1
NCT01146327 Completed Drug: PF-04620110|Drug: Placebo Healthy Pfizer|Bristol-Myers Squibb June 2010 Phase 1
NCT01064492 Completed Drug: PF-04620110 Healthy Volunteers Pfizer February 2010 Phase 1
NCT00959426 Completed Drug: PF-04620110|Drug: Placebo Obesity|Overweight|Healthy Pfizer|Bristol-Myers Squibb August 2009 Phase 1
NCT00799006 Completed Drug: Placebo|Drug: PF-04620110 Overweight Pfizer November 2008 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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