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.

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.

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.

Guar gum is an orally active nonionic galactomannan polysaccharide. It is present in the endosperm of Cyamopsis tetragonolobus seeds. Guar gum reduces cholesterol levels, regulates body weight, and acts as a thickener and viscosity modifier by forming hydrogen-bonded aqueous solutions. It serves as a rate-controlling excipient in compound delivery systems, and finds applications in the food, tissue engineering, nanosensing and industrial fields.

Enlicitide (MK-0616) decanoate is an orally active macrocyclic peptide PCSK9 inhibitor. Enlicitide decanoate binds to PCSK9, blocks its interaction with low-density lipoprotein receptor (LDLR), and enhances hepatic clearance of LDL-C. Enlicitide decanoate reduces atherogenic lipoproteins, including non-HDL cholesterol, apolipoprotein B, and lipoprotein (a). Enlicitide decanoate is applicable to research related to hypercholesterolemia, heterozygous familial hypercholesterolemia, and atherosclerotic cardiovascular disease.

SQ 31906 free base is the 3α-hydroxy isomer and metabolite of Pravastatin (HY-B0165). SQ 31906 free base forms via non-enzymatic reaction under acidic conditions. Pravastatin is used in hypercholesterolemia research.

Atorvastatin lysine is an inhibitor of HMG-CoA reductase. Atorvastatin lysine can be used to study hypercholesterolemia and mixed hyperlipidemia.

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.

Polyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. Polyphyllin H potently inhibits the activities of CYP1A2 (IC₅₀ = 6.44 μM, competitive), CYP2D6 (IC₅₀ = 13.88 μM, competitive) and CYP3A4 (IC₅₀ = 4.52 μM, non-competitive, time-dependent). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel.

BGT-002 (326E) is an orally active dual ACLY inhibitor and PPARα agonist. BGT-002 reduces lipogenesis by inhibiting synthesis and promoting efflux. BGT-002 demonstrates efficacy in ameliorating metabolic dysfunction-associated steatohepatitis (MASH) and improving hyperlipidemia in vivo. BGT-002 can be used for hypercholesterolemia and MASH research.

MI-883 is orally active constitutive androstane receptor (CAR) (EC₅₀ of 73 nM) agonist and pregnane X Receptor (PXR) (IC₅₀ of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol, LDL cholesterol, and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia.

Lovastatin acid (Mevinolinic acid; MSD803), an active metabolite of Lovastatin (HY-N0504), is a potent competitive HMG-CoA reductase inhibitor with a K_i of 0.6 nM. Lovastatin acid acts as a competitive inhibitor with respect to substrate HMG-CoA, interfering cholesterol synthesis. Lovastatin acid can be used for the research of hypercholesterolemia.

Terbufibrol is an orally active lipid-lowering agent. Terbufibrol inhibits hepatic Cholesterol 7 alpha-hydroxylase. Terbufibrol blocks a step between Acetate and HMG-CoA in the hepatic cholesterol synthesis process. Terbufibrol reduces serum total cholesterol, HDL, LDL, lipoprotein levels, and the cholesterol/phospholipid ratio, with dose- and sex-dependent changes in lipoprotein components. Terbufibrol exerts sustained cholesterol-lowering activity in baboons and rats. Terbufibrol can be used in research related to hypercholesterolemia.

MK-2206 free base is an orally active pan-AKT inhibitor, with IC₅₀ values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 free base inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 free base induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 free base causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 free base can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia.

F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC₅₀ of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR, feedback-activates hepatic FXR, promotes cholesterol metabolism and reduces lipid accumulation. F44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia.

Brutieridin (Compound 1) is a flavanone glycoside that can be isolated from the juice of bergamot (Citrus bergamia). Brutieridin reduces the level of NPC1L1 in intestinal epithelial cells. Brutieridin decreases cholesterol uptake by intestinal epithelial cells. Brutieridin reduces HMGR activity. Brutieridin can be used in the research of hypercholesterolemia.

Axitirome (CGS 26214) is a potent, liverselective TRβ receptor agonist and thyromimetic agent. Axitirome has demonstrated cholesterol-lowering activity.

Tiqueside (CP‐88,818) is an orally active cholesterol absorption inhibitor. Tiqueside inhibits absorption of both dietary cholesterol and endogenous cholesterol excreted into the intestinal lumen via the bile. Tiqueside can be used in the research of hypercholesterolemia.

Derpanicate is a Nicotinic acid (HY-B0143) ester. Derpanicate has antihypercholesterolaemic and/or vasodilating effects.