PF-05221304

Catalog No.S6145 Batch:S614501

Technical Data

Formula	C₂₈H₃₀N₄O₅
Molecular Weight	502.56	CAS No.	1370448-25-1
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (198.98 mM)
		Ethanol	5 mg/mL (9.94 mM)
		Water	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

PF-05221304 inhibits DNL, stimulates fatty acid oxidation, and reduces triglyceride accumulation in primary human hepatocytes.^[2]

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]

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[2]}	Animal Models male Sprague–Dawley rats Dosages 0.07 to 30 mg/kg Administration p.o.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[2]}

Animal Models
male Sprague–Dawley rats
Dosages
0.07 to 30 mg/kg
Administration
p.o.

References

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SHIPPING AND STORAGE
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