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Chemical Structure| 1109276-89-2 Chemical Structure| 1109276-89-2

Structure of PF-04620110
CAS No.: 1109276-89-2

Chemical Structure| 1109276-89-2

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

Synonyms: PF-04620110

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Product Details of PF-04620110

CAS No. :1109276-89-2
Formula : C21H24N4O4
M.W : 396.44
SMILES Code : O=C(O)C[C@H]1CC[C@H](C2=CC=C(N3CCOC4=NC=NC(N)=C4C3=O)C=C2)CC1
Synonyms :
PF-04620110
MDL No. :MFCD19443642

Safety of PF-04620110

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Transferase

    DGAT1, IC50:19 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMDMs) 50 μM 2 hours Suppressed fatty acid-induced NLRP3 inflammasome activation, reduced secretion of IL-1β and IL-18, but did not affect TNF-α secretion. PMC6834844
HT-29 cells 8 nM To evaluate the inhibitory effect of PF-04620110 on triglyceride synthesis in HT-29 cells, showing an IC50 of 8 nM. PMC4018057

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice High-fat diet (HFD)-induced diabetic Mice model Oral 3 mg/kg Once daily for 4 weeks Reduced HFD-induced plasma levels of IL-1β and IL-18, and decreased fasting and basal blood glucose levels. PMC6834844
Sprague-Dawley rats Acute lipid challenge model Oral 0.1, 1, or 10 mg/kg Single dose To assess the effect of PF-04620110 on plasma triglyceride levels in an acute lipid challenge model, showing significant reduction in plasma triglyceride levels at 2 hours post-dose. PMC4018057

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01166217 Healthy PHASE1 COMPLETED 2025-08-10 Pfizer Investigational Site, S... More >>ingapore, 188770, Singapore Less <<
NCT01064492 Healthy Volunteers PHASE1 COMPLETED 2025-03-10 Pfizer Investigational Site, B... More >>ruxelles, 1070, Belgium Less <<
NCT01474941 Healthy Phase 1 Completed - Belgium ... More >> Pfizer Investigational Site Bruxelles, Belgium, B-1070 Less <<
NCT01298518 Type 2 Diabetes Patients Phase 1 Completed - United States, California ... More >> Pfizer Investigational Site Chula Vista, California, United States, 91911 United States, Florida Pfizer Investigational Site DeLand, Florida, United States, 32720 Pfizer Investigational Site Miami Gardens, Florida, United States, 33169 Less <<
NCT00799006 Overweight Phase 1 Completed - United States, Connecticut ... More >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Less <<
NCT01298518 - Completed - -
NCT00959426 Obesity Overw... More >>eight Healthy Less << Phase 1 Completed - United States, Connecticut ... More >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Less <<
NCT01146327 Healthy Phase 1 Completed - Belgium ... More >> Pfizer Investigational Site Bruxelles, Belgium, B-1070 Singapore Pfizer Investigational Site Singapore, Singapore, 188770 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.22mL

5.04mL

2.52mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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