apoAL Inhibitors
Chemical inhibitors of apoAL function primarily by altering lipid metabolism and cholesterol synthesis, which are crucial for the protein's role in lipid transport. Simvastatin, lovastatin, atorvastatin, rosuvastatin, and pravastatin share a common mechanism as HMG-CoA reductase inhibitors. By inhibiting this enzyme, these statins decrease the synthesis of cholesterol within the liver. Reduced cholesterol levels in turn affect the lipidation of apoAL, a process necessary for its normal function in lipid transport. Without proper lipidation, apoAL cannot effectively carry out its role in shuttling lipids throughout the body. Ezetimibe contributes to this effect by inhibiting the intestinal absorption of cholesterol, thus decreasing the amount of cholesterol delivered to the liver for lipoprotein formation and, consequently, potentially inhibiting the functional activity of apoAL.
Fenofibrate and gemfibrozil, as PPARα agonists, induce a reduction in triglycerides and an increase in HDL cholesterol. This shift in lipid profiles can lead to a decreased availability of triglycerides for apoAL, thereby inhibiting its normal function in lipid transport. Cholestyramine further assists in this process by sequestering bile acids in the intestine, compelling the liver to convert more cholesterol into bile acids, thus depleting the cholesterol available for apoAL's lipidation. Nicotinic acid lowers the hepatic synthesis of triglycerides and VLDL, which are precursors to LDL, the primary lipoprotein that apoAL is associated with, thereby inhibiting its functional activity. Lastly, PCSK9 inhibitors like alirocumab and evolocumab increase LDL clearance by enhancing LDL receptor recycling. This reduces LDL particle availability for interaction with apoAL, which can inhibit the protein's ability to transport lipids. Collectively, these chemical inhibitors disrupt various points of lipid metabolism and cholesterol homeostasis, which are essential for the functional activity of apoAL in lipid transport.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Simvastatin | 79902-63-9 | sc-200829 sc-200829A sc-200829B sc-200829C | 50 mg 250 mg 1 g 5 g | $31.00 $89.00 $135.00 $443.00 | 13 | |
Simvastatin inhibits HMG-CoA reductase, which can lead to decreased synthesis of cholesterol. Since apoAL is involved in lipid transport and metabolism, reduced cholesterol synthesis can indirectly decrease the lipidation of apoAL, leading to its functional inhibition. | ||||||
Fenofibrate | 49562-28-9 | sc-204751 | 5 g | $41.00 | 9 | |
Fenofibrate activates PPARα, which alters the expression of genes involved in lipid metabolism. This activation can lead to an increased catabolism of triglycerides, thereby possibly reducing the availability of lipids for apoAL and inhibiting its function in lipid transport. | ||||||
Nicotinic Acid | 59-67-6 | sc-205768 sc-205768A | 250 g 500 g | $62.00 $124.00 | 1 | |
Nicotinic acid, also known as niacin, can reduce the hepatic synthesis of triglycerides, which decreases the secretion of VLDL and subsequent conversion to LDL. This reduction in available lipoproteins can inhibit the lipid transport function of apoAL. | ||||||
Gemfibrozil | 25812-30-0 | sc-204764 sc-204764A | 5 g 25 g | $66.00 $267.00 | 2 | |
Gemfibrozil acts as a PPARα agonist, similar to fenofibrate, which induces a shift in lipid metabolism that can decrease triglyceride levels and increase HDL cholesterol. This shift can indirectly inhibit apoAL's role in lipid transport due to altered lipid availability. | ||||||
Ezetimibe | 163222-33-1 | sc-205690 sc-205690A | 25 mg 100 mg | $96.00 $241.00 | 12 | |
Ezetimibe specifically inhibits the intestinal absorption of cholesterol. This leads to a decrease in the delivery of cholesterol to the liver, potentially inhibiting the lipidation of apoAL and its subsequent lipid transport activity. | ||||||
CHOLESTYRAMINE RESIN | 11041-12-6 | sc-507509 | 5 g | $210.00 | ||
Cholestyramine binds to bile acids in the intestine, preventing their reabsorption. This forces the liver to use more cholesterol to produce bile acids, which can decrease the pool of cholesterol available for lipidation of apoAL. | ||||||
Lovastatin | 75330-75-5 | sc-200850 sc-200850A sc-200850B | 5 mg 25 mg 100 mg | $29.00 $90.00 $339.00 | 12 | |
Lovastatin is an HMG-CoA reductase inhibitor like simvastatin and can lead to a decrease in cholesterol synthesis. This reduction may inhibit the functional activity of apoAL by reducing its lipidation process. | ||||||
Atorvastatin | 134523-00-5 | sc-337542A sc-337542 | 50 mg 100 mg | $257.00 $505.00 | 9 | |
Atorvastatin inhibits HMG-CoA reductase, leading to a decrease in cholesterol biosynthesis. Lower cholesterol levels can result in reduced lipidation of apoAL, indirectly inhibiting its function in lipid transport. | ||||||
Rosuvastatin | 287714-41-4 | sc-481834 | 10 mg | $145.00 | 8 | |
Rosuvastatin, another statin, inhibits HMG-CoA reductase, thereby reducing cholesterol synthesis. This can inhibit apoAL function by affecting the lipid composition of lipoproteins that apoAL interacts with. | ||||||
Pravastatin, Sodium Salt | 81131-70-6 | sc-203218 sc-203218A sc-203218B | 25 mg 100 mg 1 g | $69.00 $162.00 $787.00 | 2 | |
Pravastatin inhibits HMG-CoA reductase, ultimately leading to decreased cholesterol levels. This can indirectly inhibit the lipid transport function of apoAL by impacting its lipidation state. | ||||||