An inhibitor of ACC1 and 2
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PF-05175157

Item No. 21778

Technical Information
Formal Name
1,4-dihydro-1'-[(2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-spiro[5H-indazole-5,4'-piperidin]-7(6H)-one
CAS Number
1301214-47-0
Molecular Formula
C23H27N5O2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/ml
λmax
212, 249 nm
SMILES
CC(N1[H])=NC2=C1C=C(C(N3CCC4(CC(C=NN5C(C)C)=C5C(C4)=O)CC3)=O)C=C2
InChi Code
InChI=1S/C23H27N5O2/c1-14(2)28-21-17(13-24-28)11-23(12-20(21)29)6-8-27(9-7-23)22(30)16-4-5-18-19(10-16)26-15(3)25-18/h4-5,10,13-14H,6-9,11-12H2,1-3H3,(H,25,26)
InChi Key
BDXXSFOJPYSYOC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PF-05175157 is an inhibitor of acetyl-CoA carboxylase 1 (ACC1) and ACC2 (IC50s = 27, 33, 23.5, and 50.4 nM for human ACC1, human ACC2, rat ACC1, and rat ACC2, respectively).1 It inhibits formation of malonyl-CoA in primary rat hepatocytes (EC50 = 29.9 nM). In vivo, PF-05175157 inhibits formation of malonyl-CoA in the liver and skeletal muscle, inhibits hepatic de novo lipogenesis, and lowers the respiratory exchange rate in rats (ED50s = 6, 11, 7.8, and 3.5 mg/kg, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Griffith, D.A., Kung, D.W., Esler, W.P., et alDecreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes. J. Med. Chem. 57(24), 10512-10526 (2014).