Dyslipidemia|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Dyslipidemia is a medical condition that refers to an abnormal level of blood lipids. In developed countries, most dyslipidemias are hyperlipidemias; that is, an elevation of lipids in the blood. This is often due to diet and lifestyle. Prolonged elevation of insulin levels can also lead to dyslipidemia. Likewise, increased levels of O-GlcNAc transferase (OGT) may cause dyslipidemia.

The most common type of dyslipidemia is hyperlipidemia or high lipid levels. Another, less common form of dyslipidemia, hypolipidemia, refers to lipid levels that are abnormally low. Dyslipidemias can affect any lipid parameter, including LDL cholesterol levels, HDL cholesterol levels, triglycerides, or a combination of these lipids.

Healthy blood lipid levels naturally vary from person to person. However, people with high levels of LDL and triglycerides or very low HDL levels tend to have a higher risk of developing atherosclerosis.

Atherosclerosis develops when hard, fatty deposits called plaques accumulate in blood vessels, making it difficult for blood to flow.

Over time, these plaques can build up and cause major circulation problems, such as heart attacks and strokes.

Cat. No.	Product Name	CAS No.	Information
H6658	Ro 48-8071 fumarate	189197-69-1	A potent 2,3-oxidosqualene cyclase (OSC) inhibitor with IC50 of 6.5 nM; 6 times less potent against hamster and Gottingen minipig liver OSC, and 10-times more potent against squirrel monkey liver OSC; blocks human liver OSC and cholesterol synthesis in HepG2 cells in the nanomolar range; triggers the production of monooxidosqualene, dioxidosqualene, and epoxycholesterol.
H6657	Ro 48-8071	161582-11-2	A potent 2,3-oxidosqualene cyclase (OSC) inhibitor with IC50 of 6.5 nM; 6 times less potent against hamster and Gottingen minipig liver OSC, and 10-times more potent against squirrel monkey liver OSC; blocks human liver OSC and cholesterol synthesis in HepG2 cells in the nanomolar range; triggers the production of monooxidosqualene, dioxidosqualene, and epoxycholesterol.
H6470	Lapaquistat	189060-13-7	A novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM; displays no effect on plasma aspartate aminotransferase and alanine aminotransferase activities; effectively inhibits cholesterol synthesis in rat liver with ED50 of 2.9 mg/kg (p.o.), lowers plasma total cholesterol, triglyceride and phospholipid levels in rabbits, also inhibits the secretion of cholesterol, triglyceride and phospholipid components of very-low-density lipoprotein (VLDL) from liver.
H6167	Avasimibe	166518-60-1	Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM; potently reduces plasma cholesterol in chow-fed rats and in rabbits fed a cholesterol-free, casein-containing diet characterized by both hepatic overproduction of apo B-containing lipoproteins and delayed lipoprotein clearance; decreases both VLDL and LDL apolipoprotein B production in miniature pigs; synergistically reduces cholesteryl ester content in THP-1 macrophages combined with Atorvastatin,
H6048	TAP-311	1149362-88-8	TAP-311 is a novel potent and selective CETP inhibitor with plasma IC50 of 62 nM; displays >170-fold selectivity over CYPs, and has excellent pharmacokinetics in rats and robust efficacy in hamsters; shows substantially reduced lipophilicity with only modest distribution into adipose tissue, and retains potency in hypertriglyceridemic plasma in vitro and in vivo; does not increase blood pressure or plasma aldosterone levels in vivo, in contrast to torcetrapib.
H6047	Obicetrapib	866399-87-3	Obicetrapib (AMG-899, TA-8995, DEX-001) is a potent, ora cholesteryl ester transfer protein (CETP) inhibitor for treatment of dyslipidaemia.
H6046	Evacetrapib	1186486-62-3	Evacetrapib (LY2484595) is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) with IC50 of 5.5 nM for human recombinant CETP protein; inhibits CETP activity in human plasma with IC50 of 36 nM; shows no significant inhibition in the CEREP cell surface receptor screening, as well as the nuclear receptor panel; exhibits an ex vivo CETP inhibition ED50 of < 5 mg/kg at 8 h post oral dose and significantly elevates HDL cholesterol in vivo; Evacetrapib is a potent and selective CETP inhibitor without torcetrapib-like off-target liabilities.
H6045	CKD-519	1402796-27-3	CKD-519 (Rocacetrapib, CKD519) is a potent, selective cholesteryl ester transfer protein (CETP) inhibitor, inhibits the CETP-mediated transfer of cholesteryl ester in human serum with IC50 of 2.3 nM; exhibites a maximum of 70%-86% inhibition of CETP activity and 25%-48% increase of HDL-C levels after two weeks of oral administration of 1, 3, or 10 mg/kg in transgenic mice expressing human CETP/apolipoprotein AI; CKD-519 (Rocacetrapib, CKD519) is being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol.
H5915	Seladelpar	851528-79-5	A potent, selective, orally bioavailable PPARδ agonist for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).
H5909	Pemafibrate	848259-27-8	A highly potent, specific PPARα agonist with EC50 of 1 nM; displays >2,000-fold selectivity for PPARα over others subtypes in a CHO cell-based transactivation assay; upregulates the expression of several fatty acid β-oxidative genes in human hepatocytes and the mouse liver; significantly induces the expression of clinically beneficial target genes (VLDLR, FGF21, ABCA1, MBL2, ENPEP) in human hepatocytes.

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