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Chemical Structure : NTE-122
Catalog No.: PC-49561Not For Human Use, Lab Use Only.
NTE-122 (NTE122) is a potent selective and competitive acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, inhibits microsomal ACAT activities of various tissues and cultured cells (HepG2 and CaCo-2), with IC50 values from 1.2 to 9.6 nM.
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NTE-122 (NTE122) is a potent selective and competitive acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, inhibits microsomal ACAT activities of various tissues and cultured cells (HepG2 and CaCo-2), with IC50 values from 1.2 to 9.6 nM.
NTE-122 displays no effect on other lipid metabolizing enzymes, such as 3-hydroxy-3-methylglutaryl-CoA reductase, acyl-CoA synthetase, cholesterol esterase, lecithin:cholesterol acyltransferase, acyl-CoA:sn-glycerol-3-phosphate acyltransferase and cholesterol 7alpha-hydroxylase up to 10 uM.
NTE-122 markedly reduced serum and liver cholesterol levels in the cholesterol diet-fed rats, with ED50 of 0.12 and 0.44 mg/kg/day, respectively.
NTE-122 significantly lowered plasma and liver cholesterol levels at more than 2 mg/kg/day in the cholesterol diet-fed rabbits.
| M.Wt | 703.83 | |
| Formula | C38H60Cl2N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Azuma Y, et al. Jpn J Pharmacol. 1998 Nov;78(3):355-64.
2. Azuma Y, et al. Jpn J Pharmacol. 1999 Feb;79(2):159-67.
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