sterol biosynthesis inhibitor

Fenpropidin (Ro-12-3049), a fungicide, is a specific inhibitor of sterol 14-reductase and biosynthesis.

AY 9944 is a specific cholesterol biosynthesis inhibitor that targets the 7-dehydrocholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). At high doses, AY 9944 also inhibits sterol Δ7-Δ8 isomerase in cultured embryos, leading to the accumulation of cholest-8-en-3β-ol[1][2][3]. Additionally, AY 9944 causes hypocholesterolemia and accumulation of 7DHC.

Fenhexamid (Elevate), a sterol biosynthesis inhibitor, shows antifungal activity against the plant pathogenic fungus. Fenhexamid is used for agriculture and is present in measurable amounts in fruits and vegetables.

Dimethomorph is a fungicide and sterol biosynthesis inhibitor that inhibits fungal cell wall formation, primarily used for the control of downy mildew and late blight. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells, with an IC₂₀ of 0.263 µM.

Peraclopone is a hypolidemic drug. It is an inhibitor of 7-Dehydrocholesterol reductase. Peraclopone potently inhibits the final step in cholesterol biosynthesis. Feeding this agent to rats leads to a rapid replacement of membrane cholesterol with its immediate precursor 7-dehydrocholesterol, and a dramatic reduction in plasma sterol concentration. Peraclopone caused a dose-dependent decrease in cholesterol and a concomitant accumulation of provitamin D3 (7-dehydrocholesterol) in the skin, which is accompanied by an increase in the plasma level of 25-hydroxyvitamin D3. Treatment with peraclopone dramatically alters membrane sterol content in many membranes including the microvillus membrane of both the jejunum and ileum. In the jejunal microvillus membrane a major change in chemical composition occurred, presumably in response to the alteration in membrane sterol. The net result was a significant decline in both the static and dynamic component of membrane fluidity.