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T8949 Sigma

Telmisartan

≥98% (HPLC), solid

Synonym: 4′[(1,4′-Dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl][1,1′-biphenyl]-2-carboxylic acid, BIBR 277

  • CAS Number 144701-48-4

  • Empirical Formula (Hill Notation) C33H30N4O2

  • Molecular Weight 514.62

  •  MDL number MFCD00918125

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Description

Biochem/physiol Actions

Telmisartan is a non-peptide AT1 angiotensin receptor antagonist.

Preparation Note

Telmisartan is soluble in DMSO at a concentration that is greater than 5 mg/ml. It is insoluble in water.

Application

Telmisartan has been used as an AT1 receptor antagonist to study its effects on mouse models of myocardial infarction. This study reported that telmisartan inhibited the CCN1 upregulation and reduced CCN2 levels atrial cardiomyocytes1. Telmisartan has also been used to evaluate its effect on the expression of CCN1 in kidney cortex of mice subjected to myocardial infarction2. Furthermore, telmisartan has been used to test its efficacy against tumor growth in mouse models of colorectal cancer3.

Features and Benefits

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is featured on the Angiotensin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Boehringer Ingelheim. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

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European Pharmacopoeia (EP) Reference Standard

Telmisartan for peak identification

European Pharmacopoeia (EP) Reference Standard

Safety & Documentation

Safety Information

WGK Germany 
2

Documents

Certificate of Analysis

Protocols & Articles

Articles

Antihypertensive Agents

Download BioFiles v7 n5 (3.18 Mb PDF) Back to Pharmaceutical Drugs and Drug Candidates homepage
Sami Barghshoon
BioFiles v7 n5, 2012, 5–20
Keywords: AGE, Antihypertensives, Biofiles, Cardiovascular, Clinical, Diuretics, Help, Pharmaceutical, Reductions, Tools, Type

Discover Bioactive Small Molecules for ADME/Tox

A significant number of drugs that fail in clinical trials have been associated with safety issues, including unexpected drug-drug interactions (DDI) or lack of efficacy due to poor pharmacokinetics....
Keywords: Absorption, Bioactive small molecules, Clinical, Metabolism

Peer-Reviewed Papers

References

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1. Atrial expression of the CCN1 and CCN2 proteins in chronic heart failure. Bonda TA, Kamiński KA, Dziemidowicz M, et al. Folia Histochem. Cytobiol. 50(1), 99-103, (2012)

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2. CCN1 expression in interleukin-6 deficient mouse kidney in experimental model of heart failure. Bonda TA, Taranta A, Kaminski KA, et al. Folia Histochem. Cytobiol. 51(1), 84-91, (2013)

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3. Altered efficacy of AT1R-targeted treatment after spontaneous cancer cell-AT1R upregulation. Ager EI, Wen SW, Chan J, et al. BMC Cancer 11, 274, (2011)

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In vitro and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. Maillard, M.P., et al. J. Pharmacol. Exp. Ther. 302, 1089-1095, (2002)

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Telmisartan: a review of its use in hypertension. Sharpe, M., et al. Drugs 61, 1501-1529, (2001)

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Relationship between healthy diet and risk of cardiovascular disease among patients on drug therapies for secondary prevention: a prospective cohort study of 31 546 high-risk individuals from 40 countries. Dehghan M, Mente A, Teo KK, et al. Circulation 126(23), 2705-12, (2012)

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Late angiotensin II receptor blockade in progressive rat mesangioproliferative glomerulonephritis: new insights into mechanisms. Villa L, Boor P, Konieczny A, et al. J. Pathol. 229(5), 672-84, (2013)

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Telmisartan attenuates the inflamed mesenteric adipose tissue in spontaneous colitis by mechanisms involving regulation of neurotensin/microRNA-155 pathway. Li Y, Zuo L, Zhu W, et al. Biochem. Pharmacol. 93(4), 461-9, (2015)

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Blood pressure in early autosomal dominant polycystic kidney disease. Schrier RW, Abebe KZ, Perrone RD, et al. N. Engl. J. Med. 371(24), 2255-66, (2014)

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A quest--halting the progression of autosomal dominant polycystic kidney disease. Ellison DH and Ingelfinger JR N. Engl. J. Med. 371(24), 2329-31, (2014)

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Angiotensin blockade in late autosomal dominant polycystic kidney disease. Torres VE, Abebe KZ, Chapman AB, et al. N. Engl. J. Med. 371(24), 2267-76, (2014)

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Systolic and diastolic blood pressure changes in relation with myocardial infarction and stroke in patients with coronary artery disease. Verdecchia P, Reboldi G, Angeli F, et al. Hypertension 65(1), 108-14, (2015)

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Systolic blood pressure target levels: evidence for benefits in stroke. Lackland DT Hypertension 65(1), 39-40, (2015)

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Distinct properties of telmisartan on agonistic activities for peroxisome proliferator-activated receptor γ among clinically used angiotensin II receptor blockers: drug-target interaction analyses. Kakuta H, Kurosaki E, Niimi T, et al. J. Pharmacol. Exp. Ther. 349(1), 10-20, (2014)

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[A fixed dose combination of telmisartan, and a thiazide diuretic in the treatment of hypertension]. Vítovec J and Slíva J Vnitr. Lek. 59(5), 397-401, (2013)

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Pharmacokinetics of angiotensin II receptor blockers in the dog following a single oral administration. Baek IH, Lee BY, Lee ES, et al. Drug Res. (Stuttg.) 63(7), 357-61, (2013)

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A comparative pharmacokinetic study of a fixed dose combination for essential hypertensive patients: a randomized crossover study in healthy human volunteers. Gorain B, Choudhury H, Halder D, et al. Drug Res. (Stuttg.) 63(4), 177-84, (2013)

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Preventing cardiovascular events with angiotensin II receptor blockers: a closer look at telmisartan and valsartan. Volpe M Expert Rev. Cardiovasc. Ther. 10(8), 1061-72, (2012)

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Telmisartan in the management of diabetic nephropathy: a contemporary view. Balakumar P, Bishnoi HK, and Mahadevan N Curr. Diabetes Rev. 8(3), 183-90, (2012)

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Telmisartan and cardioprotection. Akhrass PR and McFarlane SI Vasc. Health Risk Manag. 7, 677-83, (2011)

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Telmisartan for the reduction of cardiovascular morbidity and mortality. Verdecchia P, Angeli F, Gentile G, et al. Expert Rev. Clin. Pharmacol. 4(2), 151-61, (2011)

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Nifedipine and telmisartan for the treatment of hypertension: the TALENT study. Derosa G and Maffioli P Expert Rev. Cardiovasc. Ther. 9(12), 1499-503, (2011)

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Effects of telmisartan, irbesartan, valsartan, candesartan, and losartan on cancers in 15 trials enrolling 138,769 individuals. J. Hypertens. 29(4), 623-35, (2011)

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Combination of telmisartan plus amlodipine in the treatment of hypertension: review of results. Oigman W, Neves MF, and Gismondi RA Expert Rev. Cardiovasc. Ther. 8(11), 1509-17, (2010)

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[Comprehensive management of cardiovascular risk. Focusing on telmisartan]. Ceska R, Krutská S, Zlatohlávek L, et al. Vnitr. Lek. 56(8), 839-44, (2010)

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Acute regulation of pancreatic islet microcirculation and glycaemia by telmisartan and ramipril: discordant effects between normal and type 2 diabetic rats. Olverling A, Huang Z, Nyström T, et al. Clin. Sci. 125(9), 433-8, (2013)

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Telmisartan improves insulin resistance of skeletal muscle through peroxisome proliferator-activated receptor-δ activation. Li L, Luo Z, Yu H, et al. Diabetes 62(3), 762-74, (2013)

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Novel description of the 24-hour circadian rhythms of brachial versus central aortic blood pressure and the impact of blood pressure treatment in a randomized controlled clinical trial: The Ambulatory Central Aortic Pressure (AmCAP) Study. Williams B, Lacy PS, Baschiera F, et al. Hypertension 61(6), 1168-76, (2013)

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Telmisartan: just an antihypertensive agent? A literature review. Destro M, Cagnoni F, Dognini GP, et al. Expert Opin. Pharmacother. 12(17), 2719-35, (2011)

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Telmisartan ameliorates germ cell toxicity in the STZ-induced diabetic rat: studies on possible molecular mechanisms. Kushwaha S and Jena GB Mutat. Res. 755(1), 11-23, (2013)

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Effect of nifedipine versus telmisartan on prevention of atrial fibrillation recurrence in hypertensive patients. Du H, Fan J, Ling Z, et al. Hypertension 61(4), 786-92, (2013)

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Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process. Park J, Cho W, Cha KH, et al. Int. J. Pharm. 441(1-2), 50-5, (2013)

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Clinical effectiveness of telmisartan alone or in combination therapy for controlling blood pressure and vascular risk in the elderly. Jugdutt BI Clin. Interv. Aging 5, 403-16, (2010)

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A pilot study of telmisartan for visceral adiposity in HIV infection: the metabolic abnormalities, telmisartan, and HIV infection (MATH) trial. Lake JE, Tseng CH, and Currier JS PLoS ONE 8(3), e58135, (2013)

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Candesartan reduces the innate immune response to lipopolysaccharide in human monocytes. Ignacio M. Larrayoz et al J. Hypertens. 27, 2365-76, (2010)

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Efficacy and mechanism of angiotensin II receptor blocker treatment in experimental abdominal aortic aneurysms. Iida Y, Xu B, Schultz GM, et al. PLoS ONE 7(12), e49642, (2012)

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Telmisartan inhibits cell proliferation by blocking nuclear translocation of ProHB-EGF C-terminal fragment in colon cancer cells. Ozeki K, Tanida S, Morimoto C, et al. PLoS ONE 8(2), e56770, (2013)

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Telmisartan for the management of patients at high cardiovascular risk. Ruilope LM Curr. Med. Res. Opin. 27(8), 1673-82, (2011)

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Telmisartan exerts pleiotropic effects in endothelial cells and promotes endothelial cell quiescence and survival. Siragusa M and Sessa WC Arterioscler. Thromb. Vasc. Biol. 33(8), 1852-60, (2013)

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Effects of telmisartan and valsartan on insulin sensitivity in obese diabetic mice. Ushijima K, Takuma M, Ando H, et al. Eur. J. Pharmacol. 698(1-3), 505-10, (2013)

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Effects of telmisartan therapy on interleukin-6 and tumor necrosis factor-alpha levels: a meta-analysis of randomized controlled trials. Takagi H, Mizuno Y, Yamamoto H, et al. Hypertens. Res. 36(4), 368-73, (2013)

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Inhibition of Glutaminyl Cyclases alleviates CCL2-mediated inflammation of non-alcoholic fatty liver disease in mice. Cynis H, Kehlen A, Haegele M, et al. Int. J. Exp. Pathol. 94(3), 217-25, (2013)

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Telmisartan: a review of its use in cardiovascular disease prevention. Frampton JE Drugs 71(6), 651-77, (2011)

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Ameliorative effects of telmisartan on the inflammatory response and impaired spatial memory in a rat model of Alzheimer's disease incorporating additional cerebrovascular disease factors. Shindo T, Takasaki K, Uchida K, et al. Biol. Pharm. Bull. 35(12), 2141-7, (2012)

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Potential of the angiotensin receptor blockers (ARBs) telmisartan, irbesartan, and candesartan for inhibiting the HMGB1/RAGE axis in prevention and acute treatment of stroke. Kikuchi K, Tancharoen S, Ito T, et al. Int. J. Mol. Sci. 14(9), 18899-924, (2013)

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Pharmacokinetics, pharmacodynamics and toxicity of a combination of metoprolol succinate and telmisartan in Wistar albino rats: safety profiling. Nandi U, Karmakar S, Das AK, et al. Regul Toxicol Pharmacol 65(1), 68-78, (2013)

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Telmisartan plus amlodipine single-pill combination for the management of hypertensive patients with a metabolic risk profile (added-risk patients). Ley L and Schumacher H Curr. Med. Res. Opin. 29(1), 41-53, (2013)

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Telmisartan, an AT1 receptor blocker and a PPAR gamma activator, alleviates liver fibrosis induced experimentally by Schistosoma mansoni infection. Attia YM, Elalkamy EF, Hammam OA, et al. Parasit. Vectors 6, 199, (2013)

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Protective effect of telmisartan against oxidative damage induced by high glucose in neuronal PC12 cell. Eslami H, Sharifi AM, Rahimi H, et al. Neurosci. Lett. 558, 31-6, (2014)

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Sustained blood pressure-lowering effect of aliskiren compared with telmisartan after a single missed dose. Düsing R, Brunel P, Baek I, et al. J. Clin. Hypertens. (Greenwich.) 15(1), 41-7, (2013)

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Telmisartan/amlodipine: single-pill combination in hypertension. Moen MD Am. J. Cardiovasc. Drugs 10(6), 401-12, (2010)

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Telmisartan in incipient and overt diabetic renal disease. Schmieder RE, Bakris G, and Weir MR J. Nephrol. 24(3), 263-73, (2011)

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Telmisartan or valsartan alone or in combination with hydrochlorothiazide: a review. Lacourcière Y Clin. Exp. Hypertens. 35(1), 50-60, (2013)

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Systematic review of the effect of telmisartan on insulin sensitivity in hypertensive patients with insulin resistance or diabetes. Suksomboon N, Poolsup N, and Prasit T J. Clin. Pharm. Ther. 37(3), 319-27, (2012)

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Sirolimus produced S-shaped effect on adult polycystic kidneys after 2-year treatment. Soliman A, Zamil S, Lotfy A, et al. Transplant. Proc. 44(10), 2936-9, (2012)

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Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ. Casimiro-Garcia A, Heemstra RJ, Bigge CF, et al. Bioorg. Med. Chem. Lett. 23(3), 767-72, (2013)

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Telmisartan plus propranolol improves liver fibrosis and bile duct proliferation in the PSC-like Abcb4-/- mouse model. Mende S, Schulte S, Strack I, et al. Dig. Dis. Sci. 58(5), 1271-81, (2013)

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Abnormal amounts of intracellular calcium regulatory proteins in SHRSP.Z-Lepr(fa)/IzmDmcr rats with metabolic syndrome and cardiac dysfunction. Kagota S, Maruyama K, Tada Y, et al. Can. J. Physiol. Pharmacol. 91(2), 124-33, (2013)

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Synthesis of telmisartan impurity B. Zhao L, Xia H, and Wang ZC Pharmazie 68(6), 392-5, (2013)

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Blockade of renin angiotensin system increased resistance to STZ-induced diabetes in rats with long-term high-fat diet. Li X, Yuan L, Li J, et al. Exp. Diabetes Res. 2012, 618923, (2012)

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Ambulatory central blood pressure: a new opportunity for mechanistic and clinical cardiovascular research. Mancia G Hypertension 61(6), 1148-9, (2013)

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Targeting albuminuria in arterial hypertension and diabetes: how is it best achieved and what is its clinical relevance? Chatzikyrkou C and Menne J J. Hypertens. 31(1), 44-6, (2013)

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Does the PPAR-γ-activating property of telmisartan provide a benefit in clinical practice? Fujimura A, Ushijima K, and Ando H Hypertens. Res. 36(2), 183, (2013)

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