LDLR Inhibitor

Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a) formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys.

Anti-Mouse/Rat/Human LRP1/CD91 Antibody (11H4) is a mouse-derived IgG1 κ type antibody, targeting to mouse/rat/human LRP1/CD91. Anti-Mouse/Rat/Human LRP1/CD91 Antibody (11H4) binds to the β chain of LRP1. Anti-Mouse/Rat/Human LRP1/CD91 Antibody (11H4) can be used for western blot (WB) and other detections.

LDLRAP1-IN-1 (Compound B19) is a LDLRAP1 inhibitor and antiviral agent, with an IC₅₀ of 4.98 μM for disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 covalently modifies the C119 residue of LDLRAP1 at the LDLRAP1-LDLR binding interface, thereby disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 exhibits antiviral activity against HCoV-OC43.

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).

20-HC-Me-Pyrrolidine (compound AI-3d) is a potent Aster protein inhibitor with IC₅₀s of 0.11 μM, 0.06 μM, and 0.71 μM for Aster-A, Aster-B, and Aster-C, respectively. 20-HC-Me-Pyrrolidine blocks the ability of Asters to bind and transfer cholesterol. 20-HC-Me-Pyrrolidine also inhibits the movement of low-density lipoprotein (LDL) cholesterol to the endoplasmic reticulum (ER).

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.

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

2-Acetamidophenol (Orthocetamol) is a regulator that targets ferroptosis and glutathione metabolic pathways, is the ortho-regioisomer of Paracetamol (HY-66005). 2-Acetamidophenol has anti-atherosclerotic activity, and inhibiting total cholesterol (TC) and triglyceride (TG) in a zebrafish hyperlipidemia model with IC₅₀s for 30 μM and 40 μM, respectively. 2-Acetamidophenol upregulates the expression of glutathione synthesis-related genes (such as GCLC, GCLM, GSS) and iron ion transport genes (such as FPN1, FTH), reduces the accumulation of intracellular reactive oxygen species (ROS) and ferrous ions (Fe²⁺), and enhances the activity of glutathione peroxidase GPX4, thereby inhibiting macrophage phagocytosis of oxidized low-density lipoprotein (ox-LDL) and foam cell formation.

LSN3353871 is an orally active inhibitor of lipoprotein (a) (Lp (a)) formation, with K_d values of 756 nM (apo (a) KIV8), 605 nM (apo (a) KIV7-8), and 423 nM (apo (a) KIV5-8), respectively, and an IC₅₀ of 1.69 μM against apo (a) KIV5-8. LSN3353871 reduces circulating Lp (a) levels in transgenic mice and cynomolgus monkeys. LSN3353871 can be used in the research of atherosclerotic cardiovascular disease and calcific aortic valve disease.

Orticumab (MLDL1278A) is an antibody targeting to oxidized or malondialdehyde-modified lipoprotein (LDL). Orticumab specifically inhibits oxidized low-density lipoproteins (oxLDL). Orticumab involves in modulation of autoimmune responses against oxLDL, improves atherosclerosis in animal model. Orticumab also can be used for research of psoriasis improvement.

Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.

Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC₅₀ values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.

LDL-IN-2 (compound 3) is an antioxidant against copper mediated low-density lipoproteins (LDL) oxidation.

Gemcabene calcium (PD-72953 calcium), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.

Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) is an anti-mouse/rat/bovine VLDL-R IgG1 monoclonal antibody. Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) can specifically recognize VLDLR type-I and type-II expressed in CHO cells. Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) can be used to detect the expression of VLDLR in different cells and tissues. Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) often used in western blot experiments.

LDL-IN-3 is an anti-atherosclerotic compound extracted from patent WO/2005/039596A1, example C25 and patent US 6133467, example 3.

17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC₅₀ = 69 nM) and an androgen receptor (AR) agonist (IC₅₀ = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC₅₀ = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC₅₀= 2.7 μM) and T47D breast cancer cells (EC₅₀s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.

SGC-CK1γ-1 is a potent and selective probe for the CK1γ subfamily. SGC-CK1γ-1 can inhibit LRP6 phosphorylation levels. SGC-CK1γ-1 can selectively inhibit the CK1γ kinases in living cells and inhibit both WNT signaling and human cytomegalovirus (CMV) replication. SGC-CK1γ-1 can be used for the research of infection.

2-Acetamidophenol (Standard) is the analytical standard of 2-Acetamidophenol. This product is intended for research and analytical applications. 2-Acetamidophenol (Orthocetamol) is a regulator that targets ferroptosis and glutathione metabolic pathways, is the ortho-regioisomer of Paracetamol (HY-66005). 2-Acetamidophenol has anti-atherosclerotic activity, and inhibiting total cholesterol (TC) and triglyceride (TG) in a zebrafish hyperlipidemia model with IC₅₀s for 30 μM and 40 μM, respectively. 2-Acetamidophenol upregulates the expression of glutathione synthesis-related genes (such as GCLC, GCLM, GSS) and iron ion transport genes (such as FPN1, FTH), reduces the accumulation of intracellular reactive oxygen species (ROS) and ferrous ions (Fe²⁺), and enhances the activity of glutathione peroxidase GPX4, thereby inhibiting macrophage phagocytosis of oxidized low-density lipoprotein (ox-LDL) and foam cell formation.

LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC₅₀ of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC₅₀ values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers.