Clinical data | |
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Other names | 5α-Cholest-8(14)-en-3β-ol-15-one; 3β-Hydroxy-5α-cholest-8(14)-en-15-one |
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ChemSpider | |
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CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C27H44O2 |
Molar mass | 400.647 g·mol−1 |
3D model ( JSmol) | |
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Colestolone ( INN , USAN ), also known as 5α-cholest-8(14)-en-3β-ol-15-one, is a potent inhibitor of sterol biosynthesis which is described as a hypocholesterolemic (lipid-lowering) agent. [1] [2] [3] [4] [5] It was first reported in 1977 and was studied until at least 1988, but was never introduced for medical use. [1] [3] [4]
Colestolone has been found to significantly reduce serum levels of cholesterol both in animals and in humans. [3] [4] [5] It inhibits multiple relatively early-stage steps in cholesterol biosynthesis such as HMG-CoA reductase [6] and does not appear to affect any late-stage steps (after squalene, specifically). [5] Unlike late-stage cholesterol biosynthesis inhibitors like triparanol and azacosterol, no accumulation of sterols has been observed in animals treated with colestolone, suggesting that it does not share the toxicity of late-stage cholesterol biosynthesis inhibitors. [5]
In addition to its potent inhibition of cholesterol biosynthesis, it is notable that colestolone also happens to serve as a precursor of cholesterol, and is efficiently converted into it in rat liver homogenates and upon oral administration to rats. [5]
Clinical data | |
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Other names | 5α-Cholest-8(14)-en-3β-ol-15-one; 3β-Hydroxy-5α-cholest-8(14)-en-15-one |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C27H44O2 |
Molar mass | 400.647 g·mol−1 |
3D model ( JSmol) | |
| |
|
Colestolone ( INN , USAN ), also known as 5α-cholest-8(14)-en-3β-ol-15-one, is a potent inhibitor of sterol biosynthesis which is described as a hypocholesterolemic (lipid-lowering) agent. [1] [2] [3] [4] [5] It was first reported in 1977 and was studied until at least 1988, but was never introduced for medical use. [1] [3] [4]
Colestolone has been found to significantly reduce serum levels of cholesterol both in animals and in humans. [3] [4] [5] It inhibits multiple relatively early-stage steps in cholesterol biosynthesis such as HMG-CoA reductase [6] and does not appear to affect any late-stage steps (after squalene, specifically). [5] Unlike late-stage cholesterol biosynthesis inhibitors like triparanol and azacosterol, no accumulation of sterols has been observed in animals treated with colestolone, suggesting that it does not share the toxicity of late-stage cholesterol biosynthesis inhibitors. [5]
In addition to its potent inhibition of cholesterol biosynthesis, it is notable that colestolone also happens to serve as a precursor of cholesterol, and is efficiently converted into it in rat liver homogenates and upon oral administration to rats. [5]