1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. CL 277082

CL 277082 is a potent and selective acyl CoA:cholesterol acyltransferase (ACAT) inhibitor in microsomes. CL 277082 inhibits ACAT with IC50 values of 0.14 μM for intestinal mucosal microsomes, 0.74 μM for liver, and 1.18 μM for rat adrenal. CL 277082 is a ACAT-catalyzed cholesterol esterification and cholesterol absorption inhibitor.

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CL 277082

CL 277082 Chemical Structure

CAS No. : 96224-26-9

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Description

CL 277082 is a potent and selective acyl CoA:cholesterol acyltransferase (ACAT) inhibitor in microsomes. CL 277082 inhibits ACAT with IC50 values of 0.14 μM for intestinal mucosal microsomes, 0.74 μM for liver, and 1.18 μM for rat adrenal. CL 277082 is a ACAT-catalyzed cholesterol esterification and cholesterol absorption inhibitor[1].

In Vitro

CL 277082 inhibits ACAT in cultured smooth muscle cells (IC50 = 0.8 μM). CL 277082 does not inhibit fatty acid incorporation into triglycerides or phospholipids. CL 277082 does not inhibit other cholesterol esterifying enzymes such as lecithin:cholesterol acyltransferase (LCAT) and pancreatic cholesterol esterase[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CL 277082 is a potent inhibitor of cholesterol absorption in cholesterol-fed rats by markedly inhibiting increases in liver and serum cholesterol concentration (ED50 = 5.2 mg/kg per day) while increasing the excretion of neutral 14C-labeled sterol in the feces[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

430.57

Formula

C26H36F2N2O

CAS No.
SMILES

O=C(NC1=CC=C(F)C=C1F)N(CC2=CC=C(CC(C)(C)C)C=C2)CCCCCCC

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CL 277082
Cat. No.:
HY-129344
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