875446-37-0 | (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one

Packsize	Purity	Availability	Price	Discounted Price
1mg	98+%	in stock	$6.00	$4.00
2mg	98+%	in stock	$7.00	$5.00
5mg	98+%	in stock	$9.00	$6.00
10mg	98+%	in stock	$11.00	$8.00
25mg	98+%	in stock	$14.00	$10.00
50mg	98+%	in stock	$21.00	$15.00
1g	98%	in stock	$315.00	$221.00
5g	98%	in stock	$915.00	$641.00
10g	98%	in stock	$1,584.00	$1,109.00
25g	98%	in stock	$2,873.00	$2,011.00

Description

• Catalog Number: AB51697
• Chemical Name: (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one
• CAS Number: 875446-37-0
• Molecular Formula: C30H25F10NO3
• Molecular Weight: 637.5084
• MDL Number: MFCD16294903
• SMILES: COc1cc(F)c(cc1c1ccc(cc1CN1C(=O)O[C@@H]([C@@H]1C)c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C(F)(F)F)C(C)C

Computed Properties

• Complexity: 964
• Covalently-Bonded Unit Count: 1
• Defined Atom Stereocenter Count: 2
• Heavy Atom Count: 44
• Hydrogen Bond Acceptor Count: 13
• Rotatable Bond Count: 6
• XLogP3: 8.8

Literature

• Anacetrapib lowers LDL by increasing ApoB clearance in mildly hypercholesterolemic subjects.

  The Journal of clinical investigation 20150601

• Anacetrapib as lipid-modifying therapy in patients with heterozygous familial hypercholesterolaemia (REALIZE): a randomised, double-blind, placebo-controlled, phase 3 study.

  Lancet (London, England) 20150530

• Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes.

  The Journal of pharmacology and experimental therapeutics 20150401

• Future of cholesteryl ester transfer protein inhibitors.

  Annual review of medicine 20140101

• Tangier disease: epidemiology, pathophysiology, and management.

  American journal of cardiovascular drugs : drugs, devices, and other interventions 20121001

• Cholesteryl ester transfer protein inhibition as a strategy to reduce cardiovascular risk.

  Journal of lipid research 20120901

• Rationale for cholesteryl ester transfer protein inhibition.

  Current opinion in lipidology 20120801

• HDL and CETP Inhibition: Will This DEFINE the Future?

  Current treatment options in cardiovascular medicine 20120801

• Safety of inhibition of cholesteryl ester transfer protein with anacetrapib: the DEFINE study.

  Expert review of cardiovascular therapy 20120801

• Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects.

  British journal of clinical pharmacology 20120701

• Increasing high-density lipoprotein cholesterol by cholesteryl ester transfer protein-inhibition: a rocky road and lessons learned? The early demise of the dal-HEART programme.

  European heart journal 20120701

• An update on the clinical development of dalcetrapib (RO4607381), a cholesteryl ester transfer protein modulator that increases HDL cholesterol levels.

  Future cardiology 20120701

• Current status of CETP inhibitors in the treatment of hyperlipidemia: an update.

  Current clinical pharmacology 20120501

• Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.

  Bioorganic & medicinal chemistry letters 20120501

• On- and off-target pharmacology of torcetrapib: current understanding and implications for the structure activity relationships (SAR), discovery and development of cholesteryl ester-transfer protein (CETP) inhibitors.

  Drugs 20120305

• Changes in lipoprotein subfraction concentration and composition in healthy individuals treated with the CETP inhibitor anacetrapib.

  Journal of lipid research 20120301

• New horizons for cholesterol ester transfer protein inhibitors.

  Current atherosclerosis reports 20120201

• Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction.

  Clinical pharmacology and therapeutics 20120101

• SAR studies on the central phenyl ring of substituted biphenyl oxazolidinone-potent CETP inhibitors.

  Bioorganic & medicinal chemistry letters 20120101

• Anacetrapib, a cholesteryl ester transfer protein inhibitor.

  Expert opinion on investigational drugs 20120101

• Lipid exchange mechanism of the cholesteryl ester transfer protein clarified by atomistic and coarse-grained simulations.

  PLoS computational biology 20120101

• Regulation of reverse cholesterol transport - a comprehensive appraisal of available animal studies.

  Nutrition & metabolism 20120101

• Cholesteryl ester transfer-protein modulator and inhibitors and their potential for the treatment of cardiovascular diseases.

  Vascular health and risk management 20120101

• Mipomersen: evidence-based review of its potential in the treatment of homozygous and severe heterozygous familial hypercholesterolemia.

  Core evidence 20120101

• Patient considerations and clinical impact of cholesteryl ester transfer protein inhibitors in the management of dyslipidemia: focus on anacetrapib.

  Vascular health and risk management 20120101

• Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib.

  Drug design, development and therapy 20120101

• [Secondary coronary heart disease prevention. Will CEPT inhibitors be the next breakthrough?].

  MMW Fortschritte der Medizin 20111208

• Cholesteryl ester transfer protein inhibition in cardiovascular risk management: ongoing trials will end the confusion.

  Cardiovascular therapeutics 20111201

• Familial hypercholesterolemia: present and future management.

  Current cardiology reports 20111201

• Multidimensional profiling of plasma lipoproteins by size exclusion chromatography followed by reverse-phase protein arrays.

  Journal of lipid research 20111201

• Lack of an effect of anacetrapib on the pharmacokinetics of digoxin in healthy subjects.

  Biopharmaceutics & drug disposition 20111201

• Cholesteryl ester transfer protein inhibition to reduce cardiovascular risk: Where are we now?

  Trends in pharmacological sciences 20111201

• Update on therapies targeting HDL: the mystery continues.

  Current opinion in lipidology 20111201

• Leoligin, the major lignan from Edelweiss, activates cholesteryl ester transfer protein.

  Atherosclerosis 20111101

• Anacetrapib promotes reverse cholesterol transport and bulk cholesterol excretion in Syrian golden hamsters.

  Journal of lipid research 20111101

• Investigational CETP antagonists for hyperlipidemia and atherosclerosis prevention.

  Expert opinion on investigational drugs 20111101

• Anacetrapib: a new weapon against dyslipidemia.

  Current clinical pharmacology 20111101

• Anacetrapib: hope for CETP inhibitors?

  Cardiovascular therapeutics 20111001

• Efficacy and safety after cessation of treatment with the cholesteryl ester transfer protein inhibitor anacetrapib (MK-0859) in patients with primary hypercholesterolemia or mixed hyperlipidemia.

  American heart journal 20111001

• Different effects of compounds decreasing cholesteryl ester transfer protein activity on lipoprotein metabolism.

  Current opinion in lipidology 20110801

• Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib.

  Journal of medicinal chemistry 20110714

• Model-based development of anacetrapib, a novel cholesteryl ester transfer protein inhibitor.

  The AAPS journal 20110601

• Triglyceride-rich lipoproteins and high-density lipoprotein cholesterol in patients at high risk of cardiovascular disease: evidence and guidance for management.

  European heart journal 20110601

• The cholesterol ester transfer protein inhibitor, anacetrapib.

  Current opinion in lipidology 20110601

• [Cholesteryl ester transfer protein inhibition in the management of atherosclerotic cardiovascular disease: second act 'A rebirth of hope'].

  Revista medica de Chile 20110601

• A bivariate genome-wide approach to metabolic syndrome: STAMPEED consortium.

  Diabetes 20110401

• Preparative scale synthesis of the biaryl core of anacetrapib via a ruthenium-catalyzed direct arylation reaction: unexpected effect of solvent impurity on the arylation reaction.

  The Journal of organic chemistry 20110304

• Effect of diltiazem, a moderate CYP3A inhibitor, on the pharmacokinetics of anacetrapib, a potent cholesteryl ester transfer protein inhibitor, in healthy subjects.

  Journal of clinical pharmacology 20110301

• The DEFINE study: a bright future for CETP inhibitors?

  Expert opinion on investigational drugs 20110301

• Clinical Trials Update AHA Congress 2010.

  Cardiovascular drugs and therapy 20110201

• CETP inhibition shows promise as way to reduce cardiovascular disease risk.

  JAMA 20110112

• Trial watch: hope renewed for strategy to raise HDL cholesterol.

  Nature reviews. Drug discovery 20110101

• Anacetrapib and dalcetrapib: two novel cholesteryl ester transfer protein inhibitors.

  The Annals of pharmacotherapy 20110101

• [Novel therapy for atherosclerosis and inflammatory vascular disease].

  Nihon rinsho. Japanese journal of clinical medicine 20110101

• Cardiovascular disease and dyslipidemia: beyond LDL.

  Current pharmaceutical design 20110101

• Analysis of in vitro bioactivity data extracted from drug discovery literature and patents: Ranking 1654 human protein targets by assayed compounds and molecular scaffolds.

  Journal of cheminformatics 20110101

• Dyslipidaemia of obesity, metabolic syndrome and type 2 diabetes mellitus: the case for residual risk reduction after statin treatment.

  The open cardiovascular medicine journal 20110101

• Primary prevention of coronary heart disease: integration of new data, evolving views, revised goals, and role of rosuvastatin in management. A comprehensive survey.

  Drug design, development and therapy 20110101

• Association between the interleukin-6 promoter polymorphism -174G/C and serum lipoprotein(a) concentrations in humans.

  PloS one 20110101

• Emerging therapeutic strategies to enhance HDL function.

  Lipids in health and disease 20110101

• New insights into the mechanism of low high-density lipoprotein cholesterol in obesity.

  Lipids in health and disease 20110101

• Medical angioplasty - hope and expectations: an optimistic overview.

  Journal of family & community medicine 20110101

• Safety of anacetrapib in patients with or at high risk for coronary heart disease.

  The New England journal of medicine 20101216

• Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport.

  Journal of lipid research 20101201

• Good news for 'good' cholesterol.

  Nature 20101118

• Emerging drugs for hyperlipidemia.

  Expert opinion on emerging drugs 20100901

• Biochemical characterization of cholesteryl ester transfer protein inhibitors.

  Journal of lipid research 20100901

• Drug off-target effects predicted using structural analysis in the context of a metabolic network model.

  PLoS computational biology 20100901

• Dissociating HDL cholesterol from cardiovascular risk.

  Lancet (London, England) 20100731

• Cholesterol efflux potential and antiinflammatory properties of high-density lipoprotein after treatment with niacin or anacetrapib.

  Arteriosclerosis, thrombosis, and vascular biology 20100701

• Dalcetrapib: a review of Phase II data.

  Expert opinion on investigational drugs 20100601

• [Recent advances in the research on HDL subfraction].

  Rinsho byori. The Japanese journal of clinical pathology 20100601

• High-density lipoprotein-mediated anti-atherosclerotic and endothelial-protective effects: a potential novel therapeutic target in cardiovascular disease.

  Current pharmaceutical design 20100501

• Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys.

  Drug metabolism and disposition: the biological fate of chemicals 20100301

• Metabolism and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in humans.

  Drug metabolism and disposition: the biological fate of chemicals 20100301

• [HDL and CETP in atherogenesis].

  Deutsche medizinische Wochenschrift (1946) 20100201

• Cholesteryl ester transfer protein: at the heart of the action of lipid-modulating therapy with statins, fibrates, niacin, and cholesteryl ester transfer protein inhibitors.

  European heart journal 20100101

• Current status and future directions in lipid management: emphasizing low-density lipoproteins, high-density lipoproteins, and triglycerides as targets for therapy.

  Vascular health and risk management 20100101

• Gateways to clinical trials.

  Methods and findings in experimental and clinical pharmacology 20100101

• Anacetrapib.

  American journal of cardiovascular drugs : drugs, devices, and other interventions 20100101

• Effects of fenofibrate on lipid profiles, cholesterol ester transfer activity, and in-stent intimal hyperplasia in patients after elective coronary stenting.

  Lipids in health and disease 20100101

• Update on CETP inhibition.

  Journal of clinical lipidology 20100101

• Treatment of dyslipidemia in patients with type 2 diabetes.

  Lipids in health and disease 20100101

• High density lipoproteins-based therapies for cardiovascular disease.

  Journal of cardiovascular disease research 20100101

• The pharmacology and off-target effects of some cholesterol ester transfer protein inhibitors.

  The American journal of cardiology 20091116

• Triglycerides and HDL cholesterol: stars or second leads in diabetes?

  Diabetes care 20091101

• Design of the DEFINE trial: determining the EFficacy and tolerability of CETP INhibition with AnacEtrapib.

  American heart journal 20091001

• Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.

  British journal of clinical pharmacology 20091001

• Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents.

  Expert opinion on therapeutic patents 20090901

• Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis.

  Current opinion in investigational drugs (London, England : 2000) 20090901

• The end of the road for CETP inhibitors after torcetrapib?

  Current opinion in cardiology 20090701

• Effect of cholesteryl ester transfer protein inhibitor on vitamin E transport should be studied.

  American heart journal 20090701

• Drug discovery using chemical systems biology: identification of the protein-ligand binding network to explain the side effects of CETP inhibitors.

  PLoS computational biology 20090501

• Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.

  British journal of clinical pharmacology 20090501

• Gateways to clinical trials.

  Methods and findings in experimental and clinical pharmacology 20090401

• Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib as monotherapy and coadministered with atorvastatin in dyslipidemic patients.

  American heart journal 20090201

• Assessment of the CYP3A-mediated drug interaction potential of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy volunteers.

  Journal of clinical pharmacology 20090101

• High-density lipoprotein cholesterol: current perspective for clinicians.

  Angiology 20090101

• Raising HDL cholesterol in women.

  International journal of women's health 20090101

• Multiple-dose pharmacodynamics and pharmacokinetics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.

  Clinical pharmacology and therapeutics 20081201

• JTT-705: is there still future for a CETP inhibitor after torcetrapib?

  Expert opinion on investigational drugs 20081001

• The failure of torcetrapib: what have we learned?

  British journal of pharmacology 20080801

• Torcetrapib-induced blood pressure elevation is independent of CETP inhibition and is accompanied by increased circulating levels of aldosterone.

  British journal of pharmacology 20080801

• Anacetrapib: new hope for cholesteryl ester transfer protein inhibitors in the treatment of dyslipidemia.

  Nature clinical practice. Cardiovascular medicine 20080601

• Treating high-density lipoprotein cholesterol: a return to inhibition of cholesteryl ester transfer protein?

  Current atherosclerosis reports 20080601

• Cholesteryl ester transfer protein inhibition and HDL increase: has the dream ended?

  Expert opinion on investigational drugs 20080401

• Gateways to clinical trials.

  Methods and findings in experimental and clinical pharmacology 20080301

• HDL metabolism and CETP inhibition.

  Cardiology in review 20080101

• Effect of the cholesteryl ester transfer protein inhibitor, anacetrapib, on lipoproteins in patients with dyslipidaemia and on 24-h ambulatory blood pressure in healthy individuals: two double-blind, randomised placebo-controlled phase I studies.

  Lancet (London, England) 20071208