Hypercholesterolemia

Cholesterol (from animal) is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol (from animal) plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol (from animal) is also an endogenous estrogen-related receptor α (ERRα) agonist.

Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC₅₀s of 0.39 μM and 2.39 μM, respectively.

Cholesterol Water Soluble is a major sterol in mammals, constituting 20-25% of the structural composition of the plasma membrane. The plasma membrane is highly permeable to water but relatively impermeable to ions and protons. Cholesterol Water Soluble plays an important role in determining the fluidity and permeability characteristics of membranes and the function of transporters and signaling proteins. Cholesterol Water Soluble is also an endogenous estrogen-related receptor alpha (ERRα) agonist. Cholesterol Water Soluble can be used to study the effects of cholesterol on potassium currents in inner hair cells.
(Note: This product is a mixture of Cholesterol and Methyl-β-cyclodextrin. The product specifications below only indicate the effective content of Cholesterol.)

α-Linolenic acid (ALA (free base); C18:3 (9Z,12Z,15Z) (free base); C18:3 n-3 (free base)) is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.

Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC₅₀ of 195 nM. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

Niacin (Vitamin B3) is an orally active water-soluble B3 vitamin that is an essential nutrient for humans. Niacin (Vitamin B3) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin (Vitamin B3) is also used in the study of cardiovascular diseases.

R-IMPP (PF-00932239) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia.

3-Pyridineacetic acid is an orally active nicotinic acid analog. 3-Pyridineacetic acid enhances cholesterol oxidation in rat liver mitochondria. 3-Pyridineacetic acid inhibits Triton-induced hypercholesterolemia in rats. 3-Pyridineacetic acid can be used in research related to hypercholesterolemia.

Atorvastatin hemicalcium salt (CI-981) is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, with blood-brain barrier permeability. Atorvastatin hemicalcium salt has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium salt inhibits human SV-SMC proliferation and invasion with IC₅₀s of 0.39 μM and 2.39 μM, respectively.

Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC₅₀ of 8 nM in vitro.

p-Cresyl sulfate (p-Tolyl sulfate) is a uremic toxin, that can cause renal damage and dysfunction. p-Cresyl sulfate shows antiproliferation activity. p-Cresyl sulfate increases the protein expression of HIF-1α and VHL, decreases the protein expression of HIF-2α. p-Cresyl sulfate induces epithelial-mesenchymal transition (EMT). p-Cresyl sulfate activates the JNK and p38 MAPK signaling pathways.

Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC₅₀ of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin Calcium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.

Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks hERG current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also serve as a potential peroxisome proliferator-activated receptor γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis.

Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC₅₀s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC₅₀ of 48 nM.

KB-R7943 mesylate is a widely used inhibitor of the reverse Na⁺/Ca²⁺ exchanger (NCX_rev) with IC₅₀ of 5.7±2.1 μM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.

SPC5001 sodium is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 sodium can be used for the research of hypercholesterolemia. SPC5001 sodium sequence: 5′-TGmCTACAAAACmCmCA-3′.

Pyripyropene A is an orally active, potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC₅₀ of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo.

Ganglioside GM3 is a precursor of a-, b-, and c-series gangliosides, interacts with transmembrane receptors such as the epidermal growth factor and insulin receptors, and regulates receptor functions by creating a specialized lipid environment. Ganglioside GM3 is synthesized by GM3 synthase and can be used for the research of hypercholesterolemia.

Lomitapide (AEGR-733; BMS-201038) mesylate is an orally active microsomal triglyceride transfer protein (MTP) inhibitor and a selective mTORC1 inhibitor with lipid-lowering activity and BBB permeability. Lomitapide mesylate significantly reduces plasma LDL levels by blocking the assembly and secretion of very-low-density lipoprotein (VLDL). Lomitapide mesylate inhibits mTORC1 in an ATP-dependent manner, thereby inducing AMPK-independent autophagic cell death and suppressing cancer cell growth and apoptosis. Lomitapide mesylate also enhances tumor infiltration of CD8⁺ T cells. In addition, Lomitapide mesylate inhibits HDAC, improves endothelial function, effectively alleviates vascular inflammation and oxidative stress, and exerts neuroprotective effects in a cerebral ischemia/reperfusion injury model. Lomitapide mesylate can be used in research on related diseases such as colorectal cancer, breast cancer, melanoma, ischemic stroke, and familial hypercholesterolemia.