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Cat. No. Product Name CAS No. Information
PC-43317

MK-0354

851776-28-8 MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays; shows no interaction with any other target in a panel of over 120 other proteins; MK-0354 is a competitive inhibitor of 3H-nicotinic acid binding to hGPR109a with Ki of 505 nM, fully inhibits isoproterenol stimulated lipolysis in human adipocytes with IC50 of 3.1 uM, also is a competitive antagonist of nicotinic acid-induced MAPK signaling in cells overexpressing either mGPR109a or hGPR109a; possesses plasma FFA lowering effects in mice comparable to those of nicotinic acid, does not induce vasodilation.

Atherosclerosis

Phase 2 Discontinued

PC-42893

Anacetrapib

875446-37-0 Anacetrapib (MK 0859) is a potent, orally active cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 7.9 nM and 11.8 nM for rhCETP and C13S CETP mutant, respectively; inhibits CETP-mediated cholesterol exchange, resulting in elevated HDL-cholesterol levels and reductions in LDL-cholesterol levels, demonstrates potential to treat elevated cholesterol levels in an effort prevent cardiovascular disease.

Atherosclerosis

Phase 3 Clinical

PC-42892

Torcetrapib

262352-17-0 Torcetrapib (CP-529414) is a potent cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 37 nM; shows the potential to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.

Atherosclerosis

Phase 2 Discontinued

PC-63003

SB-435495

304694-39-1 SB-435495 is a potent, orally active inhibitor of Lp-PLA2 with IC50 of 0.06 nM; inhibits the enzyme in whole human plasma with IC50 of 3 nM; shows little interaction with other CYP450 enzymes (CYP450 IC50: 1A2>100 mM, 2C9>100 uM, 2C19>40 uM, 2D6=37 uM); effectively suppresses BRB breakdown in streptozotocin-diabetic Brown Norway rats,.

Atherosclerosis

Phase 2 Discontinued

PC-62954

K-604

217094-32-1 K-604 is a potent, selective and competitive ACAT-1 inhibitor with IC50 of 0.45 uM for human ACAT-1, displays 229-fold selectivity over ACAT-2; inhibits cholesterol esterification in human monocyte-derived macrophages with IC50 of 60 nM, enhances cholesterol efflux from THP-1 macrophages to HDL3 or apolipoprotein A-I; suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels.

Atherosclerosis

Phase 2 Clinical

PC-62403

CI-976

114289-47-3 CI-976 (PD 128042) is a potent, selective, orally bioavailable inhibitor of ACAT-1 (Acetyl-CoA acetyltransferase 1) with IC50 of 73 nM; decreases plasma total cholesterol, very low density lipoprotein (VLDL) cholesterol, LDL cholesterol, apolipoprotein B, liver cholesteryl esters, and VLDL and LDL cholesteryl ester content in rabbits.

Atherosclerosis

Discontinued

PC-70225

PD-146176

4079-26-9 A potent, selective, non-competitve inhibitor of 15-lipoxygenase (15-LOX) with Ki of 197 nM; shows no demonstrable effect on 5-LOX, 12-LOX, COX-1 or COX-2; significantly abrogates SAT1-induced ferroptosis, inhibits amyloid β protein aggregate formation without changing total levels of amyloid β precursor protein (APP) in cells stably expressing APP.

Atherosclerosis

Discontinued

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