YIC-C8-434
YIC-C8-434 is an orally active ACAT inhibitor. YIC-C8-434 selectively blocks cholesterol esterification in intestinal epithelial cells and hepatocytes without affecting the production of triglycerides or phospholipids. YIC-C8-434 effectively reduces intracellular cholesteryl ester levels and induces an increase in lipid droplet volume, exhibiting excellent cholesterol-lowering activity and safety. YIC-C8-434 disrupts the assembly of hepatitis C virus (HCV) virions, reduces HCV RNA synthesis and viral particle release. YIC-C8-434 can be used in studies related to hepatitis C virus infection.
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- Formule: C31H44N2O4
- Masse moléculaire:508.69
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
YIC-C8-434 inhibits ACAT activity in Caco2 cell microsomes with an IC50 of 63 nM[1].
YIC-C8-434 inhibits ACAT activity in HepG2 cell microsomes with an IC50 of 88 nM[1].
YIC-C8-434 (10-20 μM; 29 h) decreases the number of lipid droplets and increases their average size in Huh-7 cells[2].
YIC-C8-434 (10-20 μM; 29 h) causes a modest reduction in HCV RNA synthesis but significantly impairs assembly of infectious JFH1 HCV virions in Huh-7 cells, reducing both extracellular and intracellular virus titers by approximately 5-fold[2].
YIC-C8-434 (10-20 μM; 29 h) does not reduce the abundance of HCV proteins (core, NS5A, E2, NS3) or the lipid droplet-associated cellular protein PLIN2 in JFH1 HCV-infected Huh-7 cells[2].
YIC-C8-434 (10 μM; 29 h) does not alter the co-localization of HCV core protein with lipid droplet-associated PLIN2 or with HCV RNA replication sites in JFH1 HCV-infected Huh-7 cells[2].
YIC-C8-434 (10-20 μM; 29 h) increases the buoyant density of released JFH1 HCV virions but does not reduce their specific infectivity, while decreasing overall extracellular viral particle release in Huh-7 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh-7
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Concentration:10, 20 μM
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Incubation Time:29 h
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Result:Caused a significant decrease in the number of lipid droplets (LDs) per cell compared to mock-treated cells.
Increased average LD size to twice that of mock-treated cells, with some LDs up to 3 times larger.
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Cell Line:JFH1 genotype 2a HCV-infected Huh-7
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Concentration:10, 20 μM
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Incubation Time:29 h
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Result:Caused a modest, less marked reduction in HCV RNA levels compared to triacsin C.
Significantly lowered extracellular infectious virus titers.
Decreased intracellular infectious virus TCID50 values by about 5-fold relative to mock-treated cells.
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Cell Line:JFH1 genotype 2a HCV-infected Huh-7
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Concentration:10, 20 μM
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Incubation Time:29 h
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Result:Had very little effect on the abundance of PLIN2, HCV core, NS5A, E2, or NS3 proteins compared to DMSO-treated cells.
Detected no significant reductions in targeted protein levels.
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Cell Line:JFH1 genotype 2a HCV-infected Huh-7
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Concentration:10 μM
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Incubation Time:29 h
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Result:Did not reduce the signal intensity for PLIN2 or core.
Maintained co-localization of PLIN2 and core at the same extent as in DMSO-treated cells (Pearson correlation coefficient of 0.60).
Preserved co-localization or close proximity of dsRNA punctate replication sites to core, similar to DMSO-treated cells.
YIC-C8-434 (10-100 mg/kg/d; p.o.; daily; 7 days) significantly inhibits hepatic VLDL cholesterol secretion in normal male Sprague-Dawley rats at an oral dose of 100 mg/kg/d, without affecting triacylglycerol or phospholipid secretion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 120-150 g, hypercholesterolemia model via 0.5% cholic acid, 10% sucrose, 10% coconut oil diet)[1]
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Dosage:8.3 mg/kg/d; 17.2 mg/kg/d; 33.2 mg/kg/d
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Administration:p.o.; daily; 7 days
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Result:Reduced cholesterol absorption from 67.7% (control) to 56.1%, a 17% inhibition (p<0.01).
Reduced cholesterol absorption to 50.7% (p<0.01).
Reduced cholesterol absorption to 48.9% (p<0.01).
Chemical Information
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Masse moléculaire 508.69
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Formule C31H44N2O4
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SMILES
COC1=CC(/C=C/C(N2CCN(CC2)C3=CC(C)=C(C)C=C3)=O)=CC(OC)=C1OCCCCCCCC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Ohishi K, et al. Inhibitory 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. Biological & pharmaceutical bulletin. 2003 Aug;26(8):1125-8. [Content Brief]
[2]. Liefhebber JM, et al. Modulation of triglyceride and cholesterol ester synthesis impairs assembly of infectious hepatitis C virus. The Journal of biological chemistry. 2014 Aug 01;289(31):21276-88. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YIC-C8-434 Related Classifications
HY-138198A Related Classifications
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