Hypercholesterolemia

Cholesterol (synthetic) 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 (synthetic) 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 (synthetic) is also an endogenous estrogen-related receptor α (ERRα) agonist.

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.

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.

Enniatin B-¹³C₃₃ is the ¹³C-labeled Enniatin B (HY-N3806). Enniatin B is a Fusarium mycotoxin that acts as an ionophore to form cation-selective membrane channels, disrupt ion homeostasis and mitochondrial function, inhibit cell proliferation, and induce apoptosis, while modulating ERK, p38 MAPK, and STAT3 signaling pathways. Enniatin B is used in research on atherosclerosis, hypercholesterolemia, cervical cancer, and colon adenocarcinoma.

Azalanstat (RS-21607) dihydrochloride is an orally active lanosterol 14α-demethylase inhibitor. Azalanstat dihydrochloride exerts a cholesterol-lowering effect by inhibiting cholesterol synthesis and regulating HMG-CoA Reductase (HMGCR), and shows an additive effect when used in combination with Cholestyramine (HY-104081). Azalanstat dihydrochloride is used in the study of hypercholesterolemia.

Enlicitide northern fragment 4 is a key intermediate obtained via the retrosynthetic disconnection of Enlicitide decanoate (HY-W1126955). Enlicitide northern fragment 4 participates in the protecting-group-free biocatalytic convergent assembly of Enlicitide decanoate, an oral macrocyclic peptide PCSK9 inhibitor. Enlicitide northern fragment 4 can be used for the synthesis of Enlicitide decanoate, thereby supporting research related to hypercholesterolemia.

Cholesterol (from plant) 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 plant) 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 plant) is also an endogenous estrogen-related receptor α (ERRα) agonist.

(R,R)-PCSK9 degrader 1 is an isomer of PCSK9 degrader 1 (HY-130245). (R,R)-PCSK9 degrader 1 is a HyT-like PCSK9 degrader (IC₅₀ of 655.4 nM) , and its PCSK9-binding site does not interfere with the binding of PCSK9 to LDL receptor. (R,R)-PCSK9 degrader 1 can be used in the research of atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, and related cardiovascular and cardiometabolic diseases.

PCSK9-IN-36 is a PCSK9 inhibitor and a flavonoid glycoside derivative. PCSK9-IN-36 binds stably within the surface groove of PCSK9 through hydrophobic interactions involving its flavonoid scaffold and an electrostatic hydrogen-bonding network formed by its polar glycosidic group, thereby competitively blocking the interaction between PCSK9 and the low-density lipoprotein receptor (LDLR). PCSK9-IN-36 can be used for research on hypercholesterolemia.

Rosuvastatin-d₃ is the deuterated-labeled Rosuvastatin (HY-17504A). 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.

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.

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.

Dim16 is a dual PCSK9 inhibitor and HMG-CoAR inhibitor, with an IC₅₀ of 0.8 nM against human PCSK9 and an IC₅₀ of 146.8 μM against HMG-CoAR. Dim16 disrupts the PCSK9-LDLR protein-protein interaction, inhibits the catalytic activity of HMG-CoAR, enhances cellular uptake of extracellular LDL, and suppresses PCSK9-induced platelet aggregation. Dim16 can be used in research related to hypercholesterolemia.

Keto lovastatin (Monacolin X) is an impurity of Lovastatin (HY-N0504) and also a competitive inhibitor of HMG-CoA reductase. Keto lovastatin exerts its cholesterol-lowering effect by blocking the rate-limiting step of endogenous cholesterol synthesis. Keto lovastatin can be used in research on hypercholesterolemia and atherosclerosis, and can also serve as an impurity reference standard in the research on the production and quality control of Lovastatin.