211513-37-0 | Dalcetrapib

Packsize	Purity	Availability	Price	Discounted Price
1mg	≥98%	in stock	$63.00	$45.00
5mg	≥97%	in stock	$114.00	$80.00
10mg	≥97%	in stock	$155.00	$108.00
50mg	95%	in stock	$246.00	$172.00
100mg	95%	in stock	$435.00	$304.00
250mg	95%	in stock	$863.00	$604.00

Description

• Catalog Number: AF32565
• Chemical Name: Dalcetrapib
• CAS Number: 211513-37-0
• Molecular Formula: C23H35NO2S
• Molecular Weight: 389.5945
• MDL Number: MFCD06407886
• SMILES: CCC(CC1(CCCCC1)C(=O)Nc1ccccc1SC(=O)C(C)C)CC

Computed Properties

• Complexity: 481
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 27
• Hydrogen Bond Acceptor Count: 3
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 9
• XLogP3: 7.1

Literature

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  The Journal of pharmacology and experimental therapeutics 20150401

• Future of cholesteryl ester transfer protein inhibitors.

  Annual review of medicine 20140101

• Solubility and stability of dalcetrapib in vehicles and biological media.

  International journal of pharmaceutics 20121101

• Evidence of a drug-drug interaction linked to inhibition of ester hydrolysis by orlistat.

  Journal of cardiovascular pharmacology 20121001

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

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• Lipid and apoprotein composition of HDL in partial or complete CETP deficiency.

  Current vascular pharmacology 20120701

• Determination of dalcetrapib by liquid chromatography-tandem mass spectrometry.

  Journal of pharmaceutical and biomedical analysis 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.

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

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• Vascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial.

  European heart journal 20120401

• Cholesteryl ester transfer protein inhibition and endothelial function: enough with the surrogates.

  European heart journal 20120401

• No clinically relevant drug-drug interactions when dalcetrapib is co-administered with a monophasic oral contraceptive (Microgynon® 30).

  International journal of clinical pharmacology and therapeutics 20120401

• Monitoring Cyp2b10 mRNA expression at cessation of 2-year carcinogenesis bioassay in mouse liver provides evidence for a carcinogenic mechanism devoid of human relevance: the dalcetrapib experience.

  Toxicology and applied pharmacology 20120315

• Pharmacotherapy. Elevating HDL-cholesterol levels with dalcetrapib is safe.

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• Effect of dalcetrapib plus pravastatin on lipoprotein metabolism and high-density lipoprotein composition and function in dyslipidemic patients: results of a phase IIb dose-ranging study.

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

  Journal of lipid research 20111201

• Effect of dalcetrapib, a CETP modulator, on non-cholesterol sterol markers of cholesterol homeostasis in healthy subjects.

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• Safety and efficacy of dalcetrapib on atherosclerotic disease using novel non-invasive multimodality imaging (dal-PLAQUE): a randomised clinical trial.

  Lancet (London, England) 20111029

• Dalcetrapib: turning the tide for CETP inhibition?

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• Coronary artery disease: Dalcetrapib safely raises HDL-cholesterol level in the phase IIb dal-PLAQUE trial.

  Nature reviews. Cardiology 20110927

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

  Current opinion in lipidology 20110801

• Rationale and design of dal-PLAQUE: a study assessing efficacy and safety of dalcetrapib on progression or regression of atherosclerosis using magnetic resonance imaging and 18F-fluorodeoxyglucose positron emission tomography/computed tomography.

  American heart journal 20110801

• Utility of atherosclerosis imaging in the evaluation of high-density lipoprotein-raising therapies.

  Current atherosclerosis reports 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

• Effects of food intake on the pharmacokinetic properties of dalcetrapib: findings from three phase I, single-dose crossover studies in healthy volunteers.

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  Revista medica de Chile 20110601

• Dalcetrapib pharmacokinetics and metabolism in the cynomolgus monkey.

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• Learning lessons from Pfizer's $800 million failure.

  Nature reviews. Drug discovery 20110301

• Rationale and design of dal-VESSEL: a study to assess the safety and efficacy of dalcetrapib on endothelial function using brachial artery flow-mediated vasodilatation.

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

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

  Journal of lipid research 20101201

• Lack of clinically relevant drug-drug interactions when dalcetrapib is co-administered with ezetimibe.

  British journal of clinical pharmacology 20101201

• Good news for 'good' cholesterol.

  Nature 20101118

• Coadministration of dalcetrapib with pravastatin, rosuvastatin, or simvastatin: no clinically relevant drug-drug interactions.

  Journal of clinical pharmacology 20101001

• No clinically relevant drug-drug interactions when dalcetrapib is co-administered with atorvastatin.

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• Lack of effect of dalcetrapib on QT interval in healthy subjects following multiple dosing.

  European journal of clinical pharmacology 20100801

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• MARCO, a macrophage scavenger receptor highly expressed in rodents, mediates dalcetrapib-induced uptake of lipids by rat and mouse macrophages.

  Toxicology in vitro : an international journal published in association with BIBRA 20100401

• [HDL and CETP in atherogenesis].

  Deutsche medizinische Wochenschrift (1946) 20100201

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• Rationale and design of the dal-OUTCOMES trial: efficacy and safety of dalcetrapib in patients with recent acute coronary syndrome.

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