Identification | Back Directory | [Name]
CP 113818 | [CAS]
135025-12-6 | [Synonyms]
CP 113818 Decanamide, 2-(hexylthio)-N-(6-(methyl-2,4-bis(methylthio)-3-pyridinyl)-, (S)-
N-(2,4-Bis(methylthio)-6-methylpyridin-3-yl)-2-(hexylthio)decanoic acid amide | [Molecular Formula]
C24H42N2OS3 | [MOL File]
135025-12-6.mol | [Molecular Weight]
470.8 |
Chemical Properties | Back Directory | [Boiling point ]
566.9±50.0 °C(Predicted) | [density ]
1.07±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
11.72±0.70(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Description]
The ACAT inhibitor CP-113818 may be effective in the prevention and treatment of AD by inhibiting generation of the Abeta peptide. | [Uses]
CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease[1]. | [in vivo]
CP-113818 (0-7.1 mg/kg/day) markedly reduces amyloid pathology in a mouse model of Alzheimer's disease[1]. Animal Model: | C57BL/6, hAPP (human amyloid precursor protein) transgenic mice[1] | Dosage: | 0, 0.2, 1.6, 3.2, 4.8, and 7.1 mg/kg/day | Administration: | Via implantable slow-release biopolymer pellets, 21 days for nontransgenic mice or 60 days for hAPP mice | Result: | Reduced total cholesterol levels by 29% in the serum, hepatic free cholesterol and cholesteryl-esters were also decreased in a dose-dependent manner by up to 37% and 93%, respectively in the nontransgenic mice.
Effectively reduced cholesteryl-ester levels of hAPP mice in the absence of adrenal toxicity, reduced plaque numbers, and decreased amyloid load in a gender-independent manner in hAPP mice.
Reduced levels of “insoluble” and soluble Aβ1-40 and Aβ1-42 in the brains of hAPP transgenic mice.
Restored normal spatial learning and memory in female hAPP mice in a morris water maze test.
Reduced processing of endogenous APP but not notch or N-cadherin, without directly inhibiting β- and γ-secretase activities or Aβ aggregation in nontransgenic littermates.
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| [References]
[1] Hutter-Paier B, et al. The ACAT inhibitor CP-113,818 markedly reduces amyloid pathology in a mouse model of Alzheimer's disease. Neuron. 2004 Oct 14;44(2):227-38. DOI:10.1016/j.neuron.2004.08.043 |
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