Home Metabolism Acetyl-CoA carboxylase inhibitor PF-05221304 For research use only.

PF-05221304

Synonyms: NSC 170984, R 6238, STAT5 Inhibitor III

PF-05221304 is an orally bioavailable, liver-targeted inhibitor of acetyl-CoA carboxylase (ACC), an enzyme that catalyzes the first committed step in de novo lipogenesis (DNL).

PF-05221304 Chemical Structure

PF-05221304 Chemical Structure

CAS No. 1370448-25-1

Purity & Quality Control

PF-05221304 Related Products

Biological Activity

Description PF-05221304 is an orally bioavailable, liver-targeted inhibitor of acetyl-CoA carboxylase (ACC), an enzyme that catalyzes the first committed step in de novo lipogenesis (DNL).
Targets
ACC [1]
In vitro
In vitro

PF-05221304 inhibits DNL, stimulates fatty acid oxidation, and reduces triglyceride accumulation in primary human hepatocytes.[2]
Cell Research Cell lines Cryopreserved primary human hepatocytes
Concentrations 10 μM
Incubation Time 1 h
Method

Cryopreserved primary human hepatocytes were plated at 50,000 cells/well in a 96-well collagen-coated plate using plating media. After a 4-hour incubation, plating media was replaced with Williams E maintenance media. On the following day, PF-05221304 was dissolved in dimethyl sulfoxide (DMSO), serially diluted, and added to the cells. After a 1-hour incubation with compound or vehicle, acetate was added to each well and cells were incubated for 2 hours. Upon termination of the experiment, cells were lysed and the resulting cell lysate from each well was transferred to a 96-well, clear-bottomed isoplate and mixed with microscint-E.
In Vivo
In vivo

PF-05221304 reduces DNL and steatosis in Western diet–fed rats in vivo, showing the potential to reduce hepatic lipid accumulation and potentially lipotoxicity.[2]
Animal Research Animal Models male Sprague–Dawley rats
Dosages 0.07 to 30 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03448172 Completed
Healthy
Pfizer
 April 18 2018 Phase 1
NCT03309202 Completed
Hepatic Impairment
Pfizer
 December 19 2017 Phase 1
NCT02871037 Completed
Normal Healthy
Pfizer
 August 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 502.56 Formula

C28H30N4O5
CAS No. 1370448-25-1 SDF --
Smiles COC1=CC(=CC(=N1)C2=CC=C(C=C2)C(O)=O)C(=O)N3CCC4(CC3)CC(=O)C5=C(C4)C=N[N]5C(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (198.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble


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In vivo
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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.

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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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