An inhibitor of ACC1 and ACC2
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PF-05221304

Item No. 36856

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[6-methoxy-4-[[1,4,6,7-tetrahydro-1-(1-methylethyl)-7-oxospiro[5H-indazole-5,4′-piperidin]-1′-yl]carbonyl]-2-pyridinyl]-benzoic acid
CAS Number
1370448-25-1
Synonyms
  • Clesacostat
Molecular Formula
C28H30N4O5
Formula Weight
502.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
255, 311 nm
SMILES
O=C(C1=CC=C(C2=CC(C(N3CCC4(CC3)CC(C5=C(C4)C=NN5C(C)C)=O)=O)=CC(OC)=N2)C=C1)O
InChi Code
InChI=1S/C28H30N4O5/c1-17(2)32-25-21(16-29-32)14-28(15-23(25)33)8-10-31(11-9-28)26(34)20-12-22(30-24(13-20)37-3)18-4-6-19(7-5-18)27(35)36/h4-7,12-13,16-17H,8-11,14-15H2,1-3H3,(H,35,36)
InChi Key
LXZMHBHEXAELHH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $90

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    5 mg

    $422

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    10 mg

    $755

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    PF-05221304 is an inhibitor of acetyl-CoA carboxylase 1 (ACC1) and ACC2 (IC50s = 12.4 and 8.7 nM, respectively).1 It inhibits de novo lipid synthesis (IC50 = 61 nM) and increases fatty acid oxidation in primary human hepatocytes. PF-05221304 reduces the accumulation of triglycerides composed of de novo-derived fatty acids but not dietary essential fatty acids in primary human hepatocytes. In vivo, PF-05221304 (10 and 100 mg/kg) reduces hepatic malonyl-CoA production and de novo lipogenesis in rats. It reduces hepatic fibrosis, alanine transaminase (ALT) and aspartate aminotransferase (AST) levels, and triglyceride accumulation in a rat model of non-alcoholic steatohepatitis (NASH) induced by a choline-deficient and high-fat diet (CDAHFD).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ross, T.T., Crowley, C., Kelly, K.L., et al. Acetyl-CoA carboxylase inhibition improves multiple dimensions of NASH pathogenesis in model systems. Cell. Mol. Gastroenterol. Hepatol. 10(4), 829-851 (2020).