LDLR Inhibitor

SJ-300 is a potent and selective, orally active and brain-penetrat DKK3-LRP1 interaction inhibitor. SJ-300 restores Aβ clearance in AD models. SJ 300 binds to mLRPIV with a K_d of 7.9 μM, inhibits the DKK3 mLRPIV complex with an IC₅₀ of 3.2 μM, and does not disrupt the binding of Aβ to LRP1. SJ 300 rescues cognitive function and ameliorates neuropathology (Aβ plaque reduction ≈ 73.3 %) in vivo. SJ 300 can be employed for research in Alzheimer’s disease.

Obicetrapib (TA-8995; DEZ-001) potassium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib potassium potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib potassium can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).

FASN/SCD-IN-1 is a Silybin (HY-N0779A) derivative, an orally active inhibitor of Fatty Acid Synthase (FASN)/Stearoyl-CoA Desaturase (SCD). FASN/SCD-IN-1 has shown in vitro activity in inhibiting lipid deposition, reducing FASN and SCD transcriptional levels, and exhibiting antioxidant, anti-inflammatory, and anti-fibrotic activities. FASN/SCD-IN-1 has demonstrated significant hepatoprotective effects in a rat model of acute liver injury. FASN/SCD-IN-1 ameliorates the pathological features of MASH liver, including steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative steatohepatitis (MASH). FASN/SCD-IN-1 can be used to study MASH.

Campestanol is a phytosterol that can be found in plant food. Campestanol lowers serum cholesterol and low-density lipoprotein. Campestanol can be used for the research of metabolic disorders.

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.

F 2833 is a lipid-lowering agent. F 2833 can reduce the levels of cholesterol, triglycerides, and plasma phospholipids. F 2833 can be used for research on diseases such as hyperlipidemia.

Obicetrapib (TA-8995; DEZ-001) sodium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib sodium potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib sodium can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).

Piceatannol 4'-O-glucoside is an antioxidant. Piceatannol 4'-O-glucoside is active against oxidation of the human LDL. Piceatannol 4'-O-glucoside can be isolated from Mexican Bamboo.

Kylo-0603 is an orally active thyroid hormone receptor β (THR-β) agonist with an EC₅₀ of 31.07 nM against human targets, and it exhibits much higher selectivity for THR-β than for THR-α. Kylo-0603 enables hepatocyte-targeted delivery via GalNAc modification. Kylo-0603 reduces serum cholesterol and low-density lipoprotein cholesterol levels. Kylo-0603 alleviates hepatic steatosis, inflammatory responses, hepatocyte ballooning, and non-alcoholic steatohepatitis activity scores. Kylo-0603 inhibits the progression of hepatic fibrosis. Kylo-0603 can be used for research on metabolic dysfunction-associated steatohepatitis (MASH).

S12340 is a a inhibitor of the oxidative modification of low-density lipoprotein and shows protective effect on cardiac cells exposed to oxidative stress.

Nicanartine, an orally active antioxidant and lipid-lowering compound, is an antiatherogenic drug. Nicanartine inhibits the oxidation of low-density lipoprotein (LDL).