An inhibitor of ACAT-1
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CI-976

Item No. 17235

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)-dodecanamide
CAS Number
114289-47-3
Synonyms
  • PD 128042
Molecular Formula
C23H39NO4
Formula Weight
393.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
SMILES
COC1=C(NC(C(C)(C)CCCCCCCCCC)=O)C(OC)=CC(OC)=C1
InChi Code
InChI=1S/C23H39NO4/c1-7-8-9-10-11-12-13-14-15-23(2,3)22(25)24-21-19(27-5)16-18(26-4)17-20(21)28-6/h16-17H,7-15H2,1-6H3,(H,24,25)
InChi Key
WAFNZAURAWBNDZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $81

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    10 mg

    $152

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    25 mg

    $357

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    50 mg

    $633

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    Product Description

    Acyl-coenzyme A:cholesterol acyltransferase 1 (ACAT-1) is a sterol O-acyltransferase that catalyzes the formation of fatty acid-cholesterol esters, an important step in lipoprotein assembly and dietary cholesterol absorption.1,2 CI-976 is a potent, selective inhibitor of ACAT-1 (IC50 = 73 nM).3,4 It is orally bioavailable and decreases plasma total cholesterol, very low density lipoprotein (VLDL) cholesterol, LDL cholesterol, apolipoprotein B, liver cholesteryl esters, and VLDL and LDL cholesteryl ester content in rabbits given a diet that induces hypercholesterolemia.5 CI-976 also diminishes atherosclerotic activity in hypercholesterolemic rabbits.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Buhman, K.K., Chen, H.C., and Farese, R.V., Jr. The enzymes of neutral lipid synthesis. The Journal of Biological Chemisty 276(44), 40369-40372 (2001).

    2. Shi, Y., and Burn, P. Lipid metabolic enzymes: Emerging drug targets for the treatment of obesity. Nat. Rev. Drug Discov. 3(8), 695-710 (2004).

    3. Field, F.J., Albright, E., and Mathur, S. Inhibition of acylcoenzyme A: cholesterol acyltransferase activity by PD128O42: Effect on cholesterol metabolism and secretion in CaCo-2 cells. Lipids 26(1), 1-8 (1991).

    4. O'Brien, P.M., Sliskovic, D.R., Blankley, C.J., et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J. Med. Chem. 37(12), 1810-1822 (1994).

    5. Krause, B.R., Pape, M.E., Kieft, K., et al. ACAT inhibition decreases LDL cholesterol in rabbits fed a cholesterol-free diet. Arterioscler. Thromb. 14(4), 598-604 (1994).

    6. Bocan, T.M.A., Mueller, S.B., Uhlendorf, P.D., et al. Comparison of CI-976, an ACAT inhibitor, and selected lipid-lowering agents for antiatherosclerotic activity in iliac-femoral and thoracic aortic lesions. Arterioscler. Thromb. 11(6), 1830-1843 (1991).