150683-30-0 | Tolvaptan

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$42.00	$29.00
5mg	95%	in stock	$67.00	$47.00
250mg	95%	in stock	$115.00	$80.00
1g	95%	in stock	$122.00	$86.00
5g	95%	in stock	$325.00	$228.00
10g	95%	in stock	$480.00	$336.00
25g	95%	in stock	$946.00	$662.00

Description

• Catalog Number: AB47786
• Chemical Name: Tolvaptan
• CAS Number: 150683-30-0
• Molecular Formula: C26H25ClN2O3
• Molecular Weight: 448.9413
• MDL Number: MFCD09838782
• SMILES: Clc1ccc2c(c1)[C@H](O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C

Computed Properties

• Complexity: 674
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 32
• Hydrogen Bond Acceptor Count: 3
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 3
• Undefined Atom Stereocenter Count: 1
• XLogP3: 4.8

Literature

• miR-122 Release in Exosomes Precedes Overt Tolvaptan-Induced Necrosis in a Primary Human Hepatocyte Micropatterned Coculture Model.

  Toxicological sciences : an official journal of the Society of Toxicology 20180101

• Editor's Highlight: Candidate Risk Factors and Mechanisms for Tolvaptan-Induced Liver Injury Are Identified Using a Collaborative Cross Approach.

  Toxicological sciences : an official journal of the Society of Toxicology 20170401

• Human Sulfotransferases Enhance the Cytotoxicity of Tolvaptan.

  Toxicological sciences : an official journal of the Society of Toxicology 20160301

• Inhibition of Human Hepatic Bile Acid Transporters by Tolvaptan and Metabolites: Contributing Factors to Drug-Induced Liver Injury?

  Toxicological sciences : an official journal of the Society of Toxicology 20160101

• A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.

  Toxicological sciences : an official journal of the Society of Toxicology 20131101

• Identification and characterization of an activating F229V substitution in the V2 vasopressin receptor in an infant with NSIAD.

  Journal of the American Society of Nephrology : JASN 20120928

• Antidiuretic hormone antagonist to reduce cystine stone formation.

  Annals of internal medicine 20120918

• [Hyponatremia : The water-intolerant patient].

  Medizinische Klinik, Intensivmedizin und Notfallmedizin 20120901

• Update on tolvaptan for the treatment of hyponatremia.

  Expert review of pharmacoeconomics & outcomes research 20120801

• Chronic administration of oral vasopressin type 2 receptor antagonist tolvaptan exerts both myocardial and renal protective effects in rats with hypertensive heart failure.

  Circulation. Heart failure 20120701

• Efficacy of oral tolvaptan in acute heart failure patients with hypotension and renal impairment.

  Journal of cardiovascular medicine (Hagerstown, Md.) 20120701

• Serum and urine responses to the aquaretic agent tolvaptan in hospitalized hyponatremic patients.

  International urology and nephrology 20120601

• Diagnosis and management of hyponatremia in cancer patients.

  The oncologist 20120601

• A comprehensive, longitudinal description of the in-hospital and post-discharge clinical, laboratory, and neurohormonal course of patients with heart failure who die or are re-hospitalized within 90 days: analysis from the EVEREST trial.

  Heart failure reviews 20120501

• Syndrome of inappropriate secretion of antidiuretic hormone in traumatic brain injury: when tolvaptan becomes a life saving drug.

  Journal of neurology, neurosurgery, and psychiatry 20120501

• Efficacy and tolerance of urea compared with vaptans for long-term treatment of patients with SIADH.

  Clinical journal of the American Society of Nephrology : CJASN 20120501

• [A case of venlafaxine-induced syndrome of inappropriate ADH secretion (SIADH) - treatment with tolvaptan].

  Deutsche medizinische Wochenschrift (1946) 20120501

• [Diagnostics and new treatment methods of syndrome of inappropriate antidiuretic hormone secretion (SIADH)].

  Ugeskrift for laeger 20120409

• [SIADH - a 'shambles'].

  Ugeskrift for laeger 20120409

• Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects.

  British journal of clinical pharmacology 20120401

• Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men.

  Journal of cardiovascular pharmacology 20120401

• Oxytocin and vasopressin agonists and antagonists as research tools and potential therapeutics.

  Journal of neuroendocrinology 20120401

• Vaptans: a potential new approach for treating chronic hyponatremia in psychotic patients.

  Clinical schizophrenia & related psychoses 20120401

• [SIADH and vaptans].

  Annales d'endocrinologie 20120401

• Medical therapy for acute decompensated heart failure: what recent clinical trials have taught us about diuretics and vasodilators.

  Current heart failure reports 20120301

• Tolvaptan, an oral vasopressin antagonist, in the treatment of hyponatremia in cirrhosis.

  Journal of hepatology 20120301

• Polycystic kidney disease: a 2011 update.

  Current opinion in nephrology and hypertension 20120301

• Clinical course and predictive value of liver function tests in patients hospitalized for worsening heart failure with reduced ejection fraction: an analysis of the EVEREST trial.

  European journal of heart failure 20120301

• Hyponatremia, heart failure, and the role of tolvaptan.

  Postgraduate medicine 20120301

• Considerations regarding the management of hyponatraemia secondary to SIADH.

  Best practice & research. Clinical endocrinology & metabolism 20120301

• Perspectives on the management of hyponatraemia secondary to SIADH across Europe.

  Best practice & research. Clinical endocrinology & metabolism 20120301

• Revision and update on clinical practice guideline for liver cirrhosis.

  The Korean journal of hepatology 20120301

• Effect of grapefruit juice on the pharmacokinetics of tolvaptan, a non-peptide arginine vasopressin antagonist, in healthy subjects.

  European journal of clinical pharmacology 20120201

• Absolute bioavailability of tolvaptan and determination of minimally effective concentrations in healthy subjects.

  International journal of clinical pharmacology and therapeutics 20120201

• Evaluation of costs associated with tolvaptan-mediated hospital length of stay reduction among US patients with the syndrome of inappropriate antidiuretic hormone secretion, based on SALT-1 and SALT-2 trials.

  Hospital practice (1995) 20120201

• V2 vasopressin receptor (V2R) mutations in partial nephrogenic diabetes insipidus highlight protean agonism of V2R antagonists.

  The Journal of biological chemistry 20120113

• Hyponatremia and the use of vasopressin receptor antagonists in critically ill patients.

  Journal of intensive care medicine 20120101

• Tolvaptan.

  British journal of clinical pharmacology 20120101

• Massive aquaresis after tolvaptan administration and albumin infusion in a patient with alcoholic cirrhosis.

  The American journal of medicine 20120101

• Evaluation of costs associated with tolvaptan-mediated length-of-stay reduction among heart failure patients with hyponatremia in the US, based on the EVEREST trial.

  Journal of medical economics 20120101

• Mechanism-based therapeutics for autosomal dominant polycystic kidney disease: recent progress and future prospects.

  Nephron. Clinical practice 20120101

• The role of copeptin as a diagnostic and prognostic biomarker for risk stratification in the emergency department.

  BMC medicine 20120101

• [Hyponatremic syndrome].

  La Clinica terapeutica 20120101

• Preliminary report of tolvaptan treatment in Japanese patients with heart failure.

  International heart journal 20120101

• Vasopressin receptor antagonists and their role in clinical medicine.

  Indian journal of endocrinology and metabolism 20120101

• [Tolvaptan and CKD, a balance is needed: promises and problems of new drugs in a moment of crisis].

  Giornale italiano di nefrologia : organo ufficiale della Societa italiana di nefrologia 20120101

• Long-term treatment of hyponatremic patients with nephrogenic syndrome of inappropriate antidiuresis: personal experience and review of published case reports.

  Nephron. Clinical practice 20120101

• Hyponatremia in cirrhosis and end-stage liver disease: treatment with the vasopressin V₂-receptor antagonist tolvaptan.

  Digestive diseases and sciences 20120101

• Vasopressin receptor antagonist in the treatment of the syndrome of inappropriate antidiuretic hormone in general hospital practice.

  Endocrine journal 20120101

• [Hyponatremic hypervolemia in heart failure--the hot spot for vasopressin receptor antagonists?].

  Wiadomosci lekarskie (Warsaw, Poland : 1960) 20120101

• Tolvaptan for heart failure patients with volume overload.

  Cardiovascular drugs and therapy 20111201

• High sensitivity to tolvaptan in paraneoplastic syndrome of inappropriate ADH secretion (SIADH).

  Annals of oncology : official journal of the European Society for Medical Oncology 20111201

• Vasopressin V1 receptor-mediated aldosterone production as a result of selective V2 receptor antagonism: a potential explanation for the failure of tolvaptan to reduce cardiovascular outcomes in the EVEREST trial.

  European journal of heart failure 20111201

• Tolvaptan for the treatment of hyponatremia secondary to the syndrome of inappropriate antidiuretic hormone secretion.

  Expert review of cardiovascular therapy 20111201

• [Disorders of fluid and electrolyte balance].

  Deutsche medizinische Wochenschrift (1946) 20111201

• Pharmacokinetics, pharmacodynamics and safety of tolvaptan, a novel, oral, selective nonpeptide AVP V2-receptor antagonist: results of single- and multiple-dose studies in healthy Japanese male volunteers.

  Cardiovascular drugs and therapy 20111201

• Effects of tolvaptan on volume overload in Japanese patients with heart failure: results of a phase II, multicenter, randomized, double-blind, placebo-controlled, parallel-group study.

  Cardiovascular drugs and therapy 20111201

• Efficacy and safety of tolvaptan in heart failure patients with volume overload despite the standard treatment with conventional diuretics: a phase III, randomized, double-blind, placebo-controlled study (QUEST study).

  Cardiovascular drugs and therapy 20111201

• Efficacy and safety of tolvaptan in heart failure patients with sustained volume overload despite the use of conventional diuretics: a phase III open-label study.

  Cardiovascular drugs and therapy 20111201

• Phase III clinical pharmacology study of tolvaptan.

  Cardiovascular drugs and therapy 20111201

• Effects of tolvaptan on systemic and renal hemodynamic function in dogs with congestive heart failure.

  Cardiovascular drugs and therapy 20111201

• Anti-edematous effects of tolvaptan in experimental rodent models.

  Cardiovascular drugs and therapy 20111201

• Nonclinical safety profile of tolvaptan.

  Cardiovascular drugs and therapy 20111201

• Nonclinical pharmacokinetics of a new nonpeptide V2 receptor antagonist, tolvaptan.

  Cardiovascular drugs and therapy 20111201

• A multicenter, randomized, double-blind, placebo-controlled study of tolvaptan monotherapy compared to furosemide and the combination of tolvaptan and furosemide in patients with heart failure and systolic dysfunction.

  Journal of cardiac failure 20111201

• Controlling the flood gates: vaptans, furosemide and the quest for a renal protective diuresis.

  Journal of cardiac failure 20111201

• Methyl 5-chloro-2-nitro-benzoate.

  Acta crystallographica. Section E, Structure reports online 20111201

• V2 receptor antagonist; tolvaptan.

  Electrolyte & blood pressure : E & BP 20111201

• Tolvaptan inhibits ERK-dependent cell proliferation, Cl⁻ secretion, and in vitro cyst growth of human ADPKD cells stimulated by vasopressin.

  American journal of physiology. Renal physiology 20111101

• [Slow the pace of renal failure in autosomal dominant polycystic kidney disease: hopes and disappointments].

  Presse medicale (Paris, France : 1983) 20111101

• [Tolvaptan (vasopressin receptor antagonist)].

  Nihon rinsho. Japanese journal of clinical medicine 20111101

• [Tolvaptan in antidiuretic hormone secretion syndrome secondary to treatment with citalopram].

  Revista clinica espanola 20111001

• Changes in renal function during hospitalization and soon after discharge in patients admitted for worsening heart failure in the placebo group of the EVEREST trial.

  European heart journal 20111001

• Worsening kidney function in decompensated heart failure: treat the heart, don't mind the kidney.

  European heart journal 20111001

• Tolvaptan in autosomal dominant polycystic kidney disease: three years' experience.

  Clinical journal of the American Society of Nephrology : CJASN 20111001

• Renal dysfunction in acute heart failure.

  Korean circulation journal 20111001

• Neuro-endocrine regulation of blood pressure.

  Indian journal of endocrinology and metabolism 20111001

• [The efficacy and safety of tolvaptan on treating heart failure patients with hyponatremia].

  Zhonghua xin xue guan bing za zhi 20111001

• Targeting hyponatremia and hemodynamics in acute decompensated heart failure: is there a role for vasopressin antagonists?

  Current heart failure reports 20110901

• Vaptans are not the mainstay of treatment in hyponatremia: perhaps not yet.

  Kidney international 20110901

• Short-term effects of tolvaptan on renal function and volume in patients with autosomal dominant polycystic kidney disease.

  Kidney international 20110801

• The therapeutic use of vaptans for the treatment of dilutional hyponatremia.

  Journal of pharmacy practice 20110801

• [Practical approach to hyponatremia].

  Deutsche medizinische Wochenschrift (1946) 20110801

• Hyponatremia in hospitalized patients: the potential role of tolvaptan.

  Hospital practice (1995) 20110801

• Tolvaptan inhibition of desmopressin effects on coagulation factors in a patient with decreased von Willebrand factor and polycystic kidney disease.

  Blood 20110714

• Identifying patients hospitalized with heart failure at risk for unfavorable future quality of life.

  Circulation. Cardiovascular quality and outcomes 20110701

• [Heart and kidney failure combined. Trouble seldom comes alone].

  MMW Fortschritte der Medizin 20110630

• Effects of tolvaptan on physician-assessed symptoms and signs in patients hospitalized with acute heart failure syndromes: analysis from the efficacy of vasopressin antagonism in heart failure outcome study with tolvaptan (EVEREST) trials.

  American heart journal 20110601

• In vitro P-glycoprotein interactions and steady-state pharmacokinetic interactions between tolvaptan and digoxin in healthy subjects.

  Journal of clinical pharmacology 20110501

• Tolvaptan: a new therapeutic agent.

  Reviews on recent clinical trials 20110501

• Efficacy and safety of oral tolvaptan therapy in patients with the syndrome of inappropriate antidiuretic hormone secretion.

  European journal of endocrinology 20110501

• Rationale and design of the TEMPO (Tolvaptan Efficacy and Safety in Management of Autosomal Dominant Polycystic Kidney Disease and its Outcomes) 3-4 Study.

  American journal of kidney diseases : the official journal of the National Kidney Foundation 20110501

• Arginine vasopressin (AVP) and treatment with arginine vasopressin receptor antagonists (vaptans) in congestive heart failure, liver cirrhosis and syndrome of inappropriate antidiuretic hormone secretion (SIADH).

  European journal of clinical pharmacology 20110401

• Tolvaptan for the treatment of heart failure: a review of the literature.

  Expert opinion on pharmacotherapy 20110401

• [Treatment of hyponatremia: new developments and controversies].

  Deutsche medizinische Wochenschrift (1946) 20110401

• New drugs for hyponatraemia. Cost effectiveness of tolvaptan.

  BMJ (Clinical research ed.) 20110329

• Hyponatremia: vasopressin antagonists in hyponatremia: more data needed.

  Nature reviews. Nephrology 20110301

• Hyponatremia: diagnosis, complications, and management including V2 receptor antagonists.

  Current opinion in nephrology and hypertension 20110301

• Vaptans for the treatment of hyponatremia.

  Nature reviews. Endocrinology 20110301

• Effect of serum sodium concentration and tolvaptan treatment on length of hospitalization in patients with heart failure.

  American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists 20110215

• Hepatic alteration after treatment using tolvaptan.

  Farmacia hospitalaria : organo oficial de expresion cientifica de la Sociedad Espanola de Farmacia Hospitalaria 20110101

• The cardiorenal syndrome: making the connection.

  International journal of nephrology 20110101

• Differentiation of arginine vasopressin antagonistic effects by selective V2 versus dual V2/V1a receptor blockade in a preclinical heart failure model.

  American journal of therapeutics 20110101

• Therapeutic options for the management of the cardiorenal syndrome.

  International journal of nephrology 20110101

• The cardiorenal syndrome: a review.

  International journal of nephrology 20110101

• Aortocaval fistula in rat: a unique model of volume-overload congestive heart failure and cardiac hypertrophy.

  Journal of biomedicine & biotechnology 20110101

• Cardiorenal syndrome in acute heart failure syndromes.

  International journal of nephrology 20110101

• Hyponatremia and congestive heart failure: a marker of increased mortality and a target for therapy.

  International journal of nephrology 20110101

• Tolvaptan for the management of syndrome of inappropriate antidiuretic hormone secretion: lessons learned in titration of dose.

  Endocrine practice : official journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists 20110101

• Cause of seizures: Lungs, not the brain.

  Lung India : official organ of Indian Chest Society 20110101

• Pharmacological management of cardiorenal syndromes.

  International journal of nephrology 20110101

• Tolvaptan, hyponatremia, and heart failure.

  International journal of nephrology and renovascular disease 20110101

• Management of renal failure and ascites in patients with cirrhosis.

  International journal of hepatology 20110101

• Cardiovascular agents affect the tone of pulmonary arteries and veins in precision-cut lung slices.

  PloS one 20110101

• [Treatment of hyponatremia: role of vaptans].

  Der Internist 20101201

• New drugs for hyponatraemia.

  BMJ (Clinical research ed.) 20101115

• Targeting B-Raf as a treatment strategy for polycystic kidney disease.

  American journal of physiology. Renal physiology 20101101

• Hyponatremia in acute decompensated heart failure: mechanisms, prognosis, and treatment options.

  Clinical cardiology 20101101

• Arginine vasopressin receptor antagonists (vaptans): pharmacological tools and potential therapeutic agents.

  Drug discovery today 20101001

• Dyspnoea and worsening heart failure in patients with acute heart failure: results from the Pre-RELAX-AHF study.

  European journal of heart failure 20101001

• Tolvaptan: any evidence of efficacy in SIADH?

  Prescrire international 20101001

• A multicenter, open-label, dose-ranging study to exploratively evaluate the efficacy, safety, and dose-response of tolvaptan in patients with decompensated liver cirrhosis.

  Journal of gastroenterology 20100901

• Tolvaptan: a vasopressin antagonist for the management of euvolemic and hypervolemic hyponatremia.

  Expert review of clinical pharmacology 20100901

• Vasopressin receptor antagonists for the treatment of hyponatremia: systematic review and meta-analysis.

  American journal of kidney diseases : the official journal of the National Kidney Foundation 20100801

• Chronic hyponatremia impairs memory in rats: effects of vasopressin antagonist tolvaptan.

  The Journal of endocrinology 20100701

• Vasopressin-receptor antagonists.

  Future cardiology 20100701

• The assessment and treatment of water imbalance in patients with psychosis.

  Clinical schizophrenia & related psychoses 20100701

• Treatment options for hyponatremia in heart failure.

  Congestive heart failure (Greenwich, Conn.) 20100701

• The syndrome of inappropriate antidiuretic hormone: current and future management options.

  European journal of endocrinology 20100601

• Hyponatraemia: new associations and new treatments.

  European journal of endocrinology 20100601

• Hyponatremia: Prolonged use of the vasopressin antagonist tolvaptan is a safe and effective treatment for hyponatremia.

  Nature reviews. Nephrology 20100601

• Treatment of hypervolemic or euvolemic hyponatremia associated with heart failure, cirrhosis, or the syndrome of inappropriate antidiuretic hormone with tolvaptan: a clinical review.

  Clinical therapeutics 20100601

• Renal and anti-aldosterone actions of vasopressin-2 receptor antagonism and B-type natriuretic peptide in experimental heart failure.

  Circulation. Heart failure 20100501

• Causes of death and rehospitalization in patients hospitalized with worsening heart failure and reduced left ventricular ejection fraction: results from Efficacy of Vasopressin Antagonism in Heart Failure Outcome Study with Tolvaptan (EVEREST) program.

  American heart journal 20100501

• The critical link of hypervolemia and hyponatremia in heart failure and the potential role of arginine vasopressin antagonists.

  Journal of cardiac failure 20100501

• Gateways to clinical trials.

  Methods and findings in experimental and clinical pharmacology 20100501

• [Hyponatremia in heart failure: physiopathology and pharmacological approach].

  Endocrinologia y nutricion : organo de la Sociedad Espanola de Endocrinologia y Nutricion 20100501

• [Vasopressin receptor antagonists: the vaptans].

  Endocrinologia y nutricion : organo de la Sociedad Espanola de Endocrinologia y Nutricion 20100501

• Treatment of chronic hyponatremia: now we know how, but do we know when or if?

  Journal of the American Society of Nephrology : JASN 20100401

• Oral tolvaptan is safe and effective in chronic hyponatremia.

  Journal of the American Society of Nephrology : JASN 20100401

• Critical elements of clinical follow-up after hospital discharge for heart failure: insights from the EVEREST trial.

  European journal of heart failure 20100401

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  The Annals of pharmacotherapy 20100401

• Tolvaptan.

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  Therapeutische Umschau. Revue therapeutique 20091101

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  Therapeutische Umschau. Revue therapeutique 20091101

• Tolvaptan, a selective oral vasopressin V2 receptor antagonist, ameliorates podocyte injury in puromycin aminonucleoside nephrotic rats.

  Clinical and experimental nephrology 20091001

• Effects of tolvaptan on dyspnoea relief from the EVEREST trials.

  European heart journal 20090901

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