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PF-05221304

Chemical Structure : PF-05221304

CAS No.: 1370448-25-1

PF-05221304 (Clesacostat, PF 05221304)

Catalog No.: PC-72388Not For Human Use, Lab Use Only.

PF-05221304 (PF 05221304) is a novel potent, selective, liver-targeted dual acetyl-CoA carboxylase (ACC1/2) inhibitor with IC50 of 13/9 nM (hACC1/2).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-05221304 (Clesacostat) is a novel potent, selective, liver-targeted dual acetyl-CoA carboxylase (ACC1/2) inhibitor with IC50 of 13/9 nM (hACC1/2).
PF-05221304 displays no inhibition against a panel of e 5'-diphospho-glucuronosyltransferase (UGT) enzymes at 20 uM, as well as a broad panel of transporters, receptors, ion channels and enzymes, including the hERG channel.
PF-05221304 dose-dependently causes reductions in liver de novo lipogenesis (DNL) with a maximal reduction of 82% (EC50=5.4 nM) at 300 mg/kg (p.o.), weak DNL inhibition in lung and bone marrow.

Physicochemical Properties

M.Wt 502.571
Formula C28H30N4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(4-(1-isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6-methoxypyridin-2-yl)benzoic acid

References

1. Huard K, et al. J Med Chem. 2020 Oct 8;63(19):10879-10896.

2. Calle RA, et al. Nat Med. 2021 Oct;27(10):1836-1848.

3. Ross TT, et al. Cell Mol Gastroenterol Hepatol. 2020;10(4):829-851.

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