An ACAT inhibitor
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YIC-C8-434

Item No. 45487

Technical Information
Formal Name
(2E)-3-[3,5-dimethoxy-4-(octyloxy)phenyl]-1-[4-(3,4-dimethylphenyl)-1-piperazinyl]-2-propen-1-one
CAS Number
214265-97-1
Molecular Formula
C31H44N2O4
Formula Weight
Purity
≥95%
A solid
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
CCCCCCCCOC1=C(C=C(C=C1OC)/C=C/C(N2CCN(C3=CC(C)=C(C=C3)C)CC2)=O)OC
InChi Code
InChI=1S/C31H44N2O4/c1-6-7-8-9-10-11-20-37-31-28(35-4)22-26(23-29(31)36-5)13-15-30(34)33-18-16-32(17-19-33)27-14-12-24(2)25(3)21-27/h12-15,21-23H,6-11,16-20H2,1-5H3/b15-13+
InChi Key
YGEPYVAQKIHLFY-FYWRMAATSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    YIC-C8-434 is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT; IC50 = 11 nM in isolated rat hepatic microsomes).1 It reduces plasma cholesterol levels by 79% in rats when administered at a dose of 0.005% in a high-cholesterol diet. Oral administration of YIC-C8-434 (8.3 mg/kg per day) reduces cholesterol absorption by the small intestine by 17% in rats.2 YIC-C8-434 is primarily metabolized by the cytochrome P450 (CYP) isoform CYP3A2, which is expressed at lower levels in the female rat liver, and is selectively toxic to female rats, where it reduces food intake, weight gain, and organ weights.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ohishi, K., Aiyama, R., Hatano, H., et alStructure-activity relationships of N-(3,5-dimethoxy-4-n-octyloxycinnamoyl)-N'-(3,4-dimethylphenyl)piperazine and analogues as inhibitors of acyl-CoA: cholesterol O-acyltransferase. Chem. Pharm. Bull. (Tokyo) 49(7), 830-839 (2001).

    2. Ohishi, K., Sawada, H., Yoshida, Y., et alInhibitory effects of N-(3,5-dimethoxy-4-n-octyloxycinnamoyl)-N'-(3,4-dimethylphenyl)piperazine (YIC-C8-434), an acyl-CoA: Cholesterol O-acyltransferase inhibitor, on cholesterol esterification in the intestine and liver. Biol. Pharm. Bull. 26(8), 1125-1128 (2003).

    3. Kaneko, K., Uchida, K., Kobayashi, T., et alSex-dependent toxicity of a novel acyl-CoA:cholesterol acyltransferase inhibitor, YIC-C8-434, in relation to sex-specific forms of cytochrome P450 in rats. Toxicol. Sci. 64(2), 259-268 (2001).