PF-05221304 tromethamine 

PF-05221304 tromethamine is an orally active, liver-directed and dual ACC1/ACC2 inhibitor with IC₅₀s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2. PF-05221304 tromethamine is a substrate for organic anion transport polypeptides. PF-05221304 tromethamine directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors^[1].

IC₅₀: 7.5 nM for rat ACC1, 8.2 nM for rat ACC2^[1]

PF-05221304 tromethamine inhibits hepatic de novo lipogenesis (DNL) with an IC₅₀ of 61 nM in human hepatocytes (donor HH AA 508) in a concentration-dependent manner. PF-05221304 tromethamine stimulates fatty acid oxidation and reduces triglyceride accumulation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-05221304 (5 mg/kg; p.o.; twice a day; 6 weeks) tromethamine reduces the expression of these genes (a-SMA, Col1A1, Col3A1, CCL2 and CCL11), which increases by pre-treatment with choline-deficient and high-fat diet (CDAHFD). It shows chronic administration of PF-05221304 tromethamine decreases hepatic inflammation and fibrosis in choline-deficient and high-fat diet-fed rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

623.71

C₃₂H₄₁N₅O₈

2334472-62-5

O=C(O)C=1C=CC(=CC1)C2=NC(OC)=CC(=C2)C(=O)N3CCC4(CC(=O)C5=C(C=NN5C(C)C)C4)CC3.OCC(N)(CO)CO

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Trenton T Ross, et al. Acetyl-CoA Carboxylase Inhibition Improves Multiple Dimensions of NASH Pathogenesis in Model Systems. Cell Mol Gastroenterol Hepatol. 2020;10(4):829-851.  [Content Brief]