PF-04620110

Catalog No.S7192

PF-04620110 Chemical Structure

Molecular Weight(MW): 396.44

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

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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

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

Solubility (25°C)

In vitro DMSO 49 mg/mL warmed (123.6 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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 powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01474941 Completed Healthy Pfizer June 2011 Phase 1
NCT01298518 Completed Type 2 Diabetes Patients Pfizer February 2011 Phase 1
NCT01166217 Completed Healthy Pfizer|Bristol-Myers Squibb July 2010 Phase 1
NCT01146327 Completed Healthy Pfizer|Bristol-Myers Squibb June 2010 Phase 1
NCT01064492 Completed Healthy Volunteers Pfizer February 2010 Phase 1
NCT00959426 Completed Obesity|Overweight|Healthy Pfizer|Bristol-Myers Squibb August 2009 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

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID