Bloqueadores Beta

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),

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 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 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 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),

Stability Hygroscopic
Applications An intermediate in the production of Rosuvastatin (R700500) derivatives.

Stability Light Sensitive
Applications Ciprofibrate Ethyl Ester is an impurity of ciprofibrate(C482475) is a hypolipemic agent, related structurally to Clofibrate (C586910). Ciprofibrate is used as an antilipemic.
References Davison, C., et al.: Drug. Metab. Dispos., 3, 520 (1975), Arnold, A., et al.: J. Pharm. Sci., et al.: 68, 1557 (1979), Tuchman-Duplessis, H., et al.: Toxicology, 12, 1 (1979),

Impurity Nicardipine USP Related Compound B
Applications A pyridine metabolite M-5 of Nicardipine. Nicardipine USP Related Compound B.
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 Triggle, A., et al.: J. Med. Chem., 23, 1442 (1980), Freedman, D., et al.: Drugs, 34, 578 (1987), Guengerich, F., et al.: Xenobiotica, 25, 689 (1995), Schleifer, K., et al.: Pharmazie, 54, 804 (1999),

Impurity Bisoprolol EP Impurity L (Metoprolol EP Impurity C)
Stability Hygrscopic
Applications 4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]benzaldehyde (Bisoprolol EP Impurity L (Metoprolol EP Impurity C)) is a Metoprolol impurity .
References Baldwin, J.J. , et al.: J. Med. Chem., 29, 1065 (1986), Ravelet, C., et al.: J. Sep. Sci., 29, 1322 (2006),

Applications 3-(9H-Carbazol-4-yloxy)-1,2-propanediol is used in the synthesis of carvedilol, a β-adrenergic blocking agent.
References Naidu, K. et al.: Org. Chem. An Indian J., 6, 171 (2010);

Impurity Carvedilol EP Impurity C; Carvedilol Impurity C; Carvedilol USP C
Applications N-Benzyl Carvedilol (Carvedilol EP Impurity C) is an impurity of Carvedilol (C184625) and a degradation product in Carvedilol tablets.
References Karle, C., et al.: Cardiovasc. Res., 49, 361 (2001), Chen, J., et al.: Acta Cardiol. Sin., 19, 93 (2003), Xiang, T., et al.: Pharm. Res., 22, 1205 (2005),

Stability Hygroscopic
Applications An active carboxylate of Mevastatin (M340500). It is a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase with hypocholesterolemic activity. It has been shown to be effective in reducing cholesterol synthesis in vivo, and thereby in lowering cholesterol levels in blood.
References Endo, A. et al.: Atheroscler. Supp., 5, 39 (2004); Hosobuchi, M. et al.: J. Ferm. Bioeng., 76, 470 (1993);

Impurity Nadolol EP Impurity B
Stability Hygroscopic
Applications (2R,3S)-rel-Nadolol-de(N-tert-butyl)methoxy 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)

Impurity Ezetimibe Ketone (USP)
Applications Phase-I metabolite of Ezetimibe (E975000).
References Shah, V., et al: J. Pharm. Sci., 17, 1551 (2000), Van Heek, M., et al.: Br. J. Pharmacol., 134, 409 (2001), Watts, G., et al.: Clin. Sci.,103, 595 (2002), Ghosal, A., et al.: Drug Metab. Dispos., 32, 314 (2004), Sistla, R., et al.: J. Pharm. Biomed. Anal., 39, 517 (2005),

Applications Nicergoline-d3 is the labeled analogue of Nicergoline(N394550), a drug used for age-dependent cognitive impairment such as Alzheimers disease and other types of dementia.
References Caraci, F., et. al.: Brain Res., 1047, 30 (2005); Mizuno, T., et. al.: Brain Res., 1066, 78 (2005)

Applications A labelled antihypertensive. An angiotensin converting enzyme (ACE) inhibitor, converted to active, diacid metabolite.
References Teetz, V., et al.: Arzneim.-Forsch., 34, 1399 (1984), Ruggenenti, P., et al.: Lancet, 352, (1998), Bosch, J., et al.: Br. Med. J., 324, 1 (2002),

Applications Isometheptene Maleate belongs to a group of sympathomimetic amine and shows very little antihypertensive activity. Isometheptene Maleate is used as an antispasmodic drug.
References Vidrio, H. et al.: J. Pharmacol. Exp. Therap., 187, 308 (1973); Taylor, W.G. et al.: Drug Metab. Disp., 5, 564 (1977);

Applications 2-Oxo-Zoniporide is an metabolite of Zoniporide, a potent and selective inhibitor of human sodium-hydrogen exchanger isoform1(NHE-1) and protects against cardiac ischemia-reperfusion injury.
References Ross, T.W., et al.: Cardiovascular. Drug. Reviews., 21, 17 (2003); Deepak, D., et al.: Drug. Metabol. Dispos., 38, 641 (2010);

Applications AICAR is a nucleoside analogue that is able to enter nucleoside pools and is able to significantly increase levels of adenosine during periods of ATP breakdown. Adenosine-regulating agents (ARAs) have been recognized for therapeutic potential in myocardial ischemia. Cardioprotective.
References Mullane, K., et al.: Trends Cardiovasc Med., 3, 227 (1993), Browne, G.J., et al.: J. Biol. Chem., 279, 13, 12220 (2004)

Stability Moisture Sensitive
Applications Oxyfedrine acts as a vasodilator affecting the coronary base flow.
References Baraka, Y. et al.: J. Drug Res., 12, 161 (1980);

Applications An Epinephrine (E588585) derivative formed in injection solutions and eye drops during sterilization and storage of L-Epinephrine Bitartrate.
References De Mol, N.J. et al.: Pharmac. Week., 117, 1 (1982); Liu, C. et al.: Yao. Fen. Zaz., 2, 200 (1982);

Impurity Fluocinolone Acetonide EP Impurity B
Applications (6α,11β,16α,17α)-6,9-Difluoro-11-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]-3-oxoandrosta-1,4-diene-17-carboxylic Acid, is a derivative of Fluocinolone Acetonide (F455800), which is a Corticosteroid, used in dermatology to reduce skin inflammation and relieve itching.
References Sammul, et al.: J. Assoc. Off. Agric. Chem., 47, 952 (1964), Emerson, M.V., et al.: BioDrugs, 21, 245 (2007),

Applications Inhibits the enzyme HMG-CoA reductase in vitro.
References Endo, A., et al.: J. Antibiot., 32, 852 (1979), Alberts, A.W., et al.: Drug Invest., 2 (Suppl. 2), 9 (1990), Kuroda, M., et al.: Biochim. Biophys. Acta, 486, 70 (1977),

Stability Hygroscopic
Applications The optically active isomer of Carvedilol (C184625), a nonselective ß-adrenergic blocker with a1-blocking activity. 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),

Applications A labelled nonsteroidal anti-inflammatory drug (NSAID); activity resides primarily in the (S)-isomer.
References Busson, M., et al.: J. Int. Med Res., 14, 53 (1986), Meade, E.A., et al.: J. Biol. Chem., 268, 6610 (1993), Davies, N.M., et al.: Clin. Pharmacokinet., 34, 101 (1998),

Applications 2-Fluoroadenosine is a fluorinated analog of Adenoside (A280400) nucleotide.
References Long, X., et al.: J. Pharmacol. Exper. Ther., 335, 781 (2010); Ham, M., et al.: J. Pharmacol. Exper. Ther., 335, 607 (2010);

Applications Labelled Torsemide (T548750). Used as a diuretic.
References Lesne, M., et al.: In. J. Clin. Pharmacol. Ther. Toxicol., 20, 382 (1982), Brater, D.C., et al.: Clin. Pharmacol. Ther., 42, 187 (1987),

Stability Hygroscopic
Applications Labelled Mexiletine (M340800). Antiarrhythmic (class IB).
References Singh, E.M., et al.: Br. J. Pharmacol., 44, 1 (1972), Scott, K.N., et al.: Drug Metab. Dispos., 1, 506 (1973), Chew, C.Y.C., et al.: Drugs, 17, 161 (1979), Abounassif, M.A., et al.: Anal. Profiles Drug Subs., 20, 433 (1991),

Applications N6-Isopentenyladenosine has antiproliferative activity on MCF-7 breast cancer cells.
References Rajabi, M. et al.; DNA Cell Biol.; 29, 687 (2010)

Impurity Hydrochlorothiazide EP Impurity C
Applications N-[[7-(Aminosulfonyl)-6-chloro-2,3-dihydro-1,1-dioxo-4H-1,2,4-benzothiadiazin-4-yl]methyl]-6-chloro-3,4-dihydro-1,1-dioxo-2H-1,2,4-benzothiadiazine-7-sulfonamide (Hydrochlorothiazide EP Impurity C) is an impurity in bulk Hydrochlorothiazide. Dimer Impurity C.
References Daniels, S.L., et al.: J. Pharm. Sci., 70, 211 (1981), Fang, X., et al.: Pharm. Res., 14, 691 (1997),

Applications 6-Oxo Simvastatin is an analog of Simvastatin (S485000), a HMG-CoA reductase inhibitor.
References Joshua, H., et al.: J. Antibiot., 44, 366 (1991),

Rac-Diacetolol is a racemic mixture of two isomers, (+) and (-), of acebutolol. Rac-Diacetolol is used to treat bowel disease, chronic oral inflammation and cardiac arrhythmias. It is also used as an experimental solubility probe in the study of the interactions between drugs and biological membranes. Rac-Diacetolol has been shown to have a low affinity for cytochrome P450 enzymes, which are responsible for metabolizing many drugs in the body. Rac-Diacetolol has been found to reduce plasma concentrations of PCSK9 antibody in patients with inflammatory bowel disease. The drug also has anti-inflammatory properties that may be due to its inhibition of prostaglandin synthesis.

Applications 3-Hydroxy-4-(1-naphthyloxy)-butanenitrile is an intermediate in the synthesis of Nadoxolol (N201040), which is a beta-adrenergic receptor blocker.
References Kappor, M., et al.: Bioorg. Chem., 31, 259 (2003)

Applications A metabolite of Propranolol.
References Otton, S., et al.: Br. J. Clin. Pharmacol., 30, 751 (1990), Fujita, S., et al.: J. Pharmacol. Exp. Ther., 264, 226 (1993), Bichara, N., et al.: Drug Metab. Dispos., 24, 112 (1996), Tasaki, T., et al.: J. Biochem., 123, 162 (1998),

Applications (2Z)-2,3-Dehydroxy Atorvastatin is an intermediate in synthesizing (2E)-2,3-Dehydroxy Atorvastatin (D230045), which is an impurity in the synthesis of Atorvastatin (A791750).
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996);

Applications (±)-Betaxolol-d7 HCl (iso-propyl-d7) (CAS# 1219802-92-2) is a useful isotopically labeled research compound.

Stability Hygroscopic
Applications Atorvastatin impurity in bulk drug and tablets.
References Posvar, E., et al.: J. Clin. Pharmacol., 36, 728 (1996), Lea, A., et al.: Drugs, 53, 828 (1997), Miao, X., et al.: J. Chromatogr., 998, 133 (2003),

Applications An impurity in Simvastatin (S485000).
References Sankar, D. et al.: Asian J. Chem., 21, 4294 (2009); Vuletic, M. et al.: J. Pharmac. Biomed. Anal., 37, 715 (2005);

Applications 4-Methyl-1-hydrazinophthalazine is used in the synthesis of novel phthalazine derivatives as antihypertensive agents.

Applications A 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),

Applications A new known impurity of Carvedilol (C184625), published in Carvedilol USP monograph.

Applications Hexobendine is used as vasodilator (coronary).
References Rdudolph, et al.: Arzneim.-Forsch., 20, 637 (1970), Kolassa, P., et al.: Biochem. Pharmacol., 20, 490 (1971), Zommer-Urbanska, S., et al.: Pharmazie, 40, 419 (1985),

Applications (±)-Carvedilol-d4 (ethyl-d4) (CAS# 1133705-56-2) is a useful isotopically labeled research compound.

Applications Carvedilol (C184625) derivative.
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 De(2,3-dihydroxy) Nadolol Hydrochloride 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 Lodoxamide-15N2,d2 is the labelled form of Lodoxamide which is an antiallergic drug that acts as a mast cell stabilizer. It is effective in the treatment of allergic conjunctivitis and in decreasing vascular permeability.
References Ciprandi, G., et al.: Allergy, 51(12), 946-951 (1996); Bayer, Atilla., et al.: Ophthalmologica, 217(2), 119-123 (2003)

Applications Antihypertensive; antiarrhythmic (class II); antianginal; antiglaucoma agent.
References 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 Atorvastatin 2-Hydroxy Lactone
Stability Hygroscopic
Applications A metabolite of Atorvastatin, a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.

Applications Hydroxyatenolol-d7 is the isotope labelled analog of Hydroxyatenolol (H802480); a metabolite of Atenolol (A790075) which is a cardioselective β-adrenergic blocker, antihypertensive, antianginal, and antiarrhythmic (class II).
References Escher, B., et al.: Environ. Sci. Technol., 40, 7402 (2006); Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984)

Applications Pindolol (P468000) impurity.

Applications Rescinnamine is an angiotensin-converting enzyme inhibitor used as an antihypertensive drug.
References Fife, R., et al.: Brit. Med. J., 2, 1848 (1960); Balsevich, J., et al.: Planta Med., 44, 91 (1982)

Applications Pindolol (P468000) impurity.

Applications 2-(2-Methoxyethyl)phenol is used as a stabilizer in the preparation of polysiloxane based coating compounds with good stability.

Applications (S)-4-Hydroxy Propranolol is the main metabolite of (S)-Propranolol (P831795).
References Shwed, J., et al.: Xenobiotica, 22, 973 (1992), Fujita, K., et al.: Biol. Pharm. Bull., 22, 446 (1999), Walle, U., et al.: Drug Metab. Dispos., 30, 564 (2002),

Stability Hygroscopic
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 A Labelled metabolite of Carvedilol which is a multiple-action, neurohormonal antagonist that is used in the treatment of hypertension.
References Schaefer, W.H., et al.: Drug Metab. Dispos., 26, 958 (1998).

Applications Bivalirudin 1-11 Fragment is an 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)

Impurity Atenolol EP Impurity H
Applications 2-[4-[(2RS)-2-Hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]acetonitrile is an impurity of Atenolol (A790075), a cardioselective β-adrenergic blocker. Atenolol EP Impurity H
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984);

Applications (S)-(-)-Hydroxy Timolol is a metabolite of the non-selective beta-adrenergic receptor blocker, Timolol (T443710).
References Volotinen, M. et al.: Basic Clin. Pharmacol. Toxicol., 106, 302 (2010);

Applications CMPD101 is a potent and selective GRK2/3 inhibitor.
References Lowe, J.D., et al.: Mol. Pharmacol., 88, 347 (2015); Ikeda, S., et al.: PCT Int. Appl. WO 2007034846 A1 20070329. Mar 29, 2007

Applications Labelled Penbutolol (P220500). A β-adrenoceptor antagonist. Antihypertensive.
References Armstrong, D., et al.: Anal. Chem., 66, 1473 (1994), Kato, M., et al.: J. Pharm. Biomed. Anal., 30, 1845 (2003),

Applications Methyl 4-Hydroxyphenylacetate has been shown to have potent inhibitory activity against tobacco mosaic virus (TMV).
References Shen, S., Li, W., Wang, J.: Nat. Prod. Res., 27, 2286 (2013); Golovleva, L.A., et. al.:

Applications A metabolite of the antihypertensive agent, Labetalol (L096500).
References Gal, J., et al.: Res. Comm. Chem. Pathol. Pharmacol., 62, 3 (1988),

Impurity Rosuvastatin Formyl Impurity
Applications Rosuvastatin intermediate.
References Watanabe, M., et al.: Bioorg. Med. Chem., 5, 437 (1997),

Applications A metabolite of Eplerenone. Used in combination therapy for treatment of cardiovascular disorders.
References Staessen, J., et al.: J. Endocrinol., 91, 457 (1981), de Gasparo, M., et al.: J. Pharmacol. Exp. Ther., 240, 650 (1987), MacFadyen, R., et al.: Cardiovasc. Res., 35, 30 (1997),

Applications A metabolite of Propranolol.
References Otton, S., et al.: Br. J. Clin. Pharmacol., 30, 751 (1990), Fujita, S., et al.: J. Pharmacol. Exp. Ther., 264, 226 (1993), Bichara, N., et al.: Drug Metab. Dispos., 24, 112 (1996), Tasaki, T., et al.: J. Biochem., 123, 162 (1998),

Applications (±)-2'-Methylpropranolol Hydrochloride, 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 1-Chloro-3-(1H-indol-4-yloxy)-2-propanol, is an impurity of Pindolol (P468000), a mixed β-adrenergic blocker and serotonin 5HT1A-receptor antagonist. Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.
References Dreshfield, L.J., et al.: Neurochem. Res., 21, 557 (1996), Perez, V., et al.: Lancet, 349, 1594 (1997),

Applications The labelled R-enantiomer of Propranolol (P831800). β−Adrenergic blocker. Antihypertensive; antianginal; antiarrhythmic (class II).
References Bond, et al.: Nature, 213, 721 (1967), Hansteen, V., et al.: Br. Med. J., 284, 155 (1982), Diamond, S., et al.: J. Clin. Pharmacol., 28, 193 (1988),

Applications Pindolol (P468000) impurity.
References Ohia, S., et al.: Pharmacol. Exp. Ther., 255, 11 (1990), Juteau, H., et al.: Bioorg. Med. Chem., 9, 1977 (2001),

Impurity Atorvastatin lactam phenanthrene calcium salt impurity
Applications Atorvastatin (A791750) impurity. A stable Atorvastatin formulation.