Beta Blockers

Impurity Fluocinolone Acetonide EP Impurity E
Stability Hygroscopic
Applications (6α,9β,11β,16α)-9,11-Epoxy-6-fluoro-21-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]pregna-1,4-diene-3,20-dione, can be used in the production of fluocinolone acetonide (F455800).
References Grinenko, G.S, Khimiko-Farmatsevticheskii Zhurnal, 12, 110 (1978), Sammul, et al.: J. Assoc. Off. Agric. Chem., 47, 952 (1964), Emerson, M.V., et al.: BioDrugs, 21, 245 (2007),

Applications Diazoxide-d3 is the labeled analogue of Diazoxide (D417305), which reduces status epilepticus neuron damage in diabetes.
References Baba, A., et al.: J. Neurosci., 23, 7737 (2003); Bancila, V., et al.: J. Neurochem., 90, 1243 (2004); Bancila, V., et al.: J. Biol. Chem., 280, 8793 (2005)

Applications A labelled metabolite of Spironolactone.
References Gochman, N., et al.: J. Pharmacol. Exp. Ther., 135, 312 (1962), Tori, K., et al.: Steroids, 4, 713 (1964), Solymoss, B., et al.: Toxicol. Appli. Pharmacol., 18, 586 (1971),

Applications Atorvastatin (A791750) impurity.
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996);

Applications 2-[3-(Aminosulfonyl)-4-chlorobenzoyl]-benzonic Acid is a potential metabolite of Chlorthalidone.
References Salado C., et al.: J. Chromatography. Biomed. App., 690, 195 (1997);

Applications Aprindine is a long-acting antiarrhythmic agent, effective when administered orally or intravenously in the treatment of ventricular arrhythmias of varying etiologies.
References Danilo, P. Jr., et al.: Am. Heart. J., 97, 119 (1979); Atarashi, H., et al.: Circulation. J., 66, 553 (2002);

Applications 2-(2-Aminoethoxy)anisole is used as an additive to vinylphosphonic acid esters and acrylonitrile forming compounds displaying hypotensive activity. An impurity from the process of Carvedilol (C184625)
References Reznik, V. et al.: Russ. Chem. Bull., 48, 979, (1999); Hirohashi, M., et al.: Arzneim.-Forsch., 40, 735 (1990), Packer, M., et al.: N. Engl. J. Med., 334, 1349 (1996),

Applications 5-Oxorosuvastatin methyl ester is an intermediate in the synthesis of Rosuvasatatin (calcium salt: R700500), a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor that decreases high-sensitivity C-reactive protein (hsCRP) and cholesterol concentrations in the blood.
References McTaggart, F., et al.: Am. J. Cardiol., 87, 28 (2001); Ridker, P., et al.: Lancet, 373, 1175 (2009)

Applications An isomer of the antiarrhythmic, antiglaucoma agent Timolol (T443700).
References Marini, R.D. et al.: Anal. Chim. Acta, 531, 131 (2005);

Applications (2R,3S)-rel-Nadolol-N-[(2R,3S)-rel-Nadolol-de(N-tert-butyl)]is an impurity of Nadolol (N201050), a β-Adrenergic blocker. Antihypertensive; antianginal.
References Dreyfuss, J., et al.: J. Clin. Pharmacol., 17, 300 (1977); Sibley, P.L., et al.: Toxicol. Appl. Pharmacol., 44, 379 (1978); Slusarek, L., et al.: Anal. Profiles Drug Subs., 9, 455 (1980)

Applications Labelled Dopamine. Endogenous catecholamine with α and β-adrenergic activity. Cardiotonic; antihypotensive.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Carter, J.E., et al.: Anal. Profiles Drug Subs., 11, 257 (1982), Dasta, J.F., et al.: Pharmacotherapy, 6, 304 (1986),

Applications (-)-Nebivolol intermediate.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Applications A compound present in olive oil. An important fine chemical intermediate with broad prospects for application development.
References Shu, Y., et al.: Guangdong Huagong, 37, 108 (2010), Papadopoulos, G., et al.: J Am Oil Chem Soc, 68, 669 (1991),

Applications Cardioselective β-adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic (class II).
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984),

Impurity Metoprolol EP Impurity N
Applications 3-Isopropylamino-1,2-propanediol (Metoprolol EP Impurity N) is a versatile organic building block, used in different chemical synthesis. It is used in the preparation of heterocyclic propanolamines, which are shown to have β-adrenergic antagonist activity.
References Dean, V. et al.: Drug Design and Discovery,10, 89 (1993);

Applications 4-Hydroxy Flecainide is an analogue of Flecainide (F390000).
References Blom, Y., et al.: J. Chromatogr., 653, 138 (1993),

Applications An antiarrhythmic agent isolated from Rauwolfia serpentina.
References Galarreta, B., et al.: Bioorg. Med. Chem., 16, 6689 (2008), Sun, L., et al.: Plant Mol. Biol., 67, 455 (2008), Ruiz-May, E., et al.: Mol. Biotechnol., 41, 278 (2009),

Impurity Timolol EP Impurity H
Applications 2-(3-(tert-Butylamino)-2-hydroxypropyl)-4-morpholino-1,2,5-thiadiazol-3(2H)-one is a impurity of Timolol (T443710), an antihypertensive; antiarrhythmic (class II); antianginal; antiglaucoma agent.
References Lacroix, P.M., et. al.: Chirality, 6, 484 (1994); Wasson, et al.: J. Med. Chem., 15, 651 (1972); Franciosa, et al.: Clin. Pharmacol. Ther., 13, 138 (1972); Heel, R.C., et al.: Drugs, 17, 38 (1979); Rofman, B.A., et al.: Hypertension, 2, 643 (1980); Mazzo, D.J., et al.: Anal. Profiles Drug Subs., 16, 641 (1987)

Impurity Metoprolol EP Impurity A
Applications C-Desmethyl Metoprolol (Metoprolol EP Impurity A) is a new byproduct detected in Metoprolol tartrate. Metoprolol impurity.
References Erickson, M., et al.: J. Pharma. Biomed. Analysis, 13, 567 (1995), Phinney, K., et al.: Chirality, 15, 287 (2003), Zheng, J., et al.: Anal. Chem., 78, 1535 (2006),

Impurity Rosuvastatin EP Impurity G
Stability Hygroscopic
Applications ent-Rosuvastatin is an enantiomer of Rosuvastatin (R700500), an impurity which acts as a selective, competitive HMG-CoA reductase inhibitor (1). Antilipemic (2,3).
References 1. Watanabe, M. et al.: Bioorg. Med. Chem. 1997 Feb;5(2):437-44.2. Lee, E. et al.: Clin. Pharmacol. Ther. 2005 Oct;78(4):330-41.3. Ferdinand, C. et al.: Am. J. Cardiol. 2006 Jan 15;97(2):229-35.

Applications A Rosuvastatin (R700500) intermediate as HMG-CoA reductase inhibitor.
References Beck, et al.: J. Med. Chem., 33, 52 (1999),

Impurity Atenolol EP Impurity A
Applications 4-(Hydroxyphenyl)acetamide (Atenolol EP Impurity A) is used as an intermediate for the synthesis of Atenolol (A790075) and various other organic compounds and pharmaceuticals. It is a process impurity for Atenolol (A790075)
References Inkum, R., et al.: Maejo Int. J. Sci. Tech., 6, 372 (2012); Pai, N.R., et al.: J. Chem. Pharma. Rsch., 4, 375 (2012); Moon, J.T., et al.: Bio-org. Medn. Chem., 20, 734 (2012);

Impurity Verapamil EP Impurity J HCl
Applications Nor Verapamil Hydrochloride (Verapamil EP Impurity J HCl) is a metabolite of Verapamil.
References Mutlib, A.E., et al.: The Journal of Pharm. & Exp. Therapeutics, 252, 2, 593 (1989)

Stability Hygroscopic
Applications 2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-carboxylic Acid is a transformation product of Valsartan (V095750); a nonpeptide angiotensin II AT1-receptor antagonist and antihypertensive. 2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-carboxylic Acid is also referred to as Valsartan acid.
References Noedler, K., et al.: Water Res., 47, 6650 (2013); Criscione, L., et al.: Brit. J. Pharmacol., 110, 761 (1993); Muller, P., et al.: Eur. J. Clin. Pharmacol., 47, 231 (1994)

Applications An optically active metabolite of Carvedilol (C184625), a nonselective ß-adrenergic blocker with α1-blocking activity.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Sponer, G., et al.: J. Cardiovasc. Pharmacol., 9, 317 (1987), Fujimaki, M., ET AL.: Xenobiotica, 20, 1025 (1990), Ruffolo, R., et al.: Eur. J. Clin. Pharmacol., 38, S82 (1990), Schaefer, W.H., et al.: Drug Metab. Dispos., 26, 10, 958 (1998),

Impurity Atorvastatin Pyrrolidone Analog (USP)
Stability Light Sensitive
Applications A photodegradation product of Atorvastatin (a cyclic impurity of Atorvastatin). Atorvastatin Pyrrolidone Analog (USP).
References Roger, D., et al.: Clin. Exp. Dermatol., 19, 88 (1994), Cosa, G., et al.: Photochem. Photobiol., 80, 159 (2004), Kerwin, B., et al.: J. Pharm. Sci., 96, 1468 (2007),

Impurity Ezetimibe Tetrahydropyran Impurity
Applications Ezetimibe (E975000) tetrahydropyran impurity.

Applications A metabolite of Metoprolol.
References Lennard, M.S., et al.: Br. J. Clin. Pharmacol., 14, 713 (1982), Gengo, F.M., et al.: Clin. Pharmacol. Ther., 36, 320 (1984),

Stability Hygroscopic
Applications Used as an antihypertensive.This compound is very unstable in solution and will hydrolyze readily to give benazapril.

Applications Carvedilol-d5 is the labelled analog of Carvedilol, a nonselective β-adrenergic blocker with α1-blocking activity. Carvedilol is an antihypertensive used in the treatment of congestive heart failure.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Hirohashi, M., et al.: Arzneim.-Forsch., 40, 735 (1990), Packer, M., et al.: N. Engl. J. Med., 334, 1349 (1996),

Applications A vascularly inactive metabolite of Carvedilol (C184625). A novel antihypertensive agent, is a potent antioxidant.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Sponer, G., et al.: J. Cardiovasc. Pharmacol., 9, 317 (1987), Rapola, J., et al.: Lancet, 349, 1715 (1997), Gao, F., et al.: Eur. J. Pharmacol., 406, 109 (2000),

Applications A labelled metabolite of Carvedilol (C184625). It is used in the treatment of hypertension.
References Sponer, G., et al.: J. Cardiovasc. Pharmacol., 9, 317 (1987), Fujimaki, M., ET AL.: Xenobiotica, 20, 1025 (1990), Ruffolo, R., et al.: Eur. J. Clin. Pharmacol., 38, S82 (1990), Schaefer, W.H., et al.: Drug Metab. Dispos., 26, 10, 958 (1998),

Impurity Atorvastatin EP Impurity G
Applications Atorvastatin derivative.

Impurity Tranexamic EP Impurity A
Applications Tranexamic Acid Dimer (Tranexamic EP Impurity A) is a Tranexamic Acid (T714505) impurity.

Applications Impurity of Bivalirudin, a direct thrombin inhibitor acting as an anticoagulant through inhibition of the enzyme thrombin.
References Bertrand, O. et al.: Am. J. Cardio., 110, 599 (2012); Patti, G. et al.: Am. J. Cardio., 110, 478 (2012);

Applications An enantiomeric impurity of Ezetimibe (E975005), an antihyperlipoproteinemic and cholesterol absorption inhibitor.

Applications Rosuvastatin Methyl Ester is an impurity of Rosuvastatin (R700500) in the pharmaceutical dosage forms under forced degradation conditions.
References Lennernas, H., et al.: Clin. Pharmacokinet., 32, 403 (1997), Kivisto, K., et al.: Br. J. Clin. Pharmacol., 46, 49 (1998), Lan, K., et al.: J. Pharm. Biomed. Anal., 44, 540 (2007),

Applications Labelled Ouabain (O714500). A cardiac glycoside that inhibits Na(+)/K(+) ATPase. It regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Padilha, A.S. et al.: Clin. Exp. Pharmacol. Physiol., 35, 801 (2008); Blaustein, M.P. et al.: Clin. Exp. Hypertens. 20, 691 (1998); van Huysse, J.W. et al.: Clin. Exp. Hypertens. 20, 657 (1998);

Applications Edoxaban is an anticoagulant drug which acts as a direct factor Xa inhibitor.
References Ruff, C., et al.: Am. Heart J., 160, 635 (2010); Ogata, K., et al.: J. Clin. Pharm., 50, 73 (2010)

Applications β-Adrenergic blocker. Antihypertensive; antianginal.
References Dreyfuss, J., et al.: J. Clin. Pharmacol., 17, 300 (1977), Sibley, P.L., et al.: Toxicol. Appl. Pharmacol., 44, 379 (1978), Slusarek, L., et al.: Anal. Profiles Drug Subs., 9, 455 (1980),