Bêta-bloquants

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 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 Mixed β-adrenergic blocker and serotonin 5HT1A-receptor antagonist. Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.
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 Dreshfield, L. J., et al.: Neurochem. Res., 21, 557 (1996); Perez, V., et al.: Lancet, 349, 1594 (1997)

Impurity Atenolol 2-Hydroxy Impurity
Applications Hydroxyatenolol is a metabolite of Atenolol (A790075); a cardioselective β-adrenergic blocker, antihypertensive, antianginal, and antiarrhythmic (class II). Atenolol 2-Hydroxy Impurity
References Escher, B., et al.: Environ. Sci. Technol., 40, 7402 (2006); Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984)

Applications Tirofiban intermediate.

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),

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),

Applications N-Formyl Cardevilol is an impurity of Carvedilol (C184625).
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 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),

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

Impurity Carvedilol EP Impurity D; Carvedilol USP-D
Applications 4-(2,3-Epoxypropoxy)carbazole (Carvedilol EP Impurity D; Carvedilol USP-D) is an intermediate in the synthesis of Carvedilol (C184625).

Applications 2-Azidoethanol is used as a reagent in the glycosylation of mono- or polysaccharides. 2-Azidoethanol is also used as a 2’-deoxy-ethynyluridine (EdU) blocker in nuclear DNA, preventing cross reactivity with other antibodies in order to better study its related pathways in the body.
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 Liboska, R., et al.: PLOS ONE, 7, e51679 (2012); Sun, X., et al.: Biomacromolecules, 3, 1065 (2002)

Applications A metabolite of Carvedilol (C184625), a nonselective β-adrenergic blocker with α1-blocking activity.
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), Clohs, L., et al.: J. Pharm. Biomed. Anal., 31, 407 (2003),

Applications Used as an antihypertensive and antianginal.
References Gross, G.J., et al.: Gen. Pharmacol., 14, 677 (1983), Molyvdas, P.A. and Sperelakis, N.: J. Cardiovasc. Pharmacol., 8, 449 (1986), Mizuno, K., et al.: Res. Comm. Chem. Pathol. Pharmacol., 52, 3 (1986)

Stability Hygroscopic
Applications rac-4-Hydroxy Propranolol Hydrochloride is a metabolite of Propranolol.
References Walle, T., et al.: Drug Metab. Dispos., 13, 204 (1985), Mason, R., et al.: J. Med. Chem., 34, 869 (1991), Anderson, R., et al.: Biochem. Pharmacol., 52, 341 (1996), Hung, D., et al.: J. Pharmacol. Exp. Ther., 297, 780 (2001),

Impurity Diltiazem EP Impurity F
Applications Desacetyl Diltiazem (Diltiazem EP Impurity F) is a metabolite of Diltiazem (D460620).
References Shallcross, H., et al.: Br. Med. J., 295, 1236 (1987), Yeung, P.K.F., et al.: Drug Metab. Dispos., 18, 1055 (1990), Cashman, J.R., et al.: J. Med. Chem., 34,2049 (1991),

Applications Dabigatran Carboxamide Ethyl Ester is an impurity of Dabigatran Etexilate Mesylate (D100150) which is a nonpeptide, direct thrombin inhibitor.
References Hauel, N., et al.: J. Med. Chem., 45, 1757 (2002); Mungall, D., et al.: Curr. Opin. Invest. Drugs, 3, 095 (2002); Stangier, J., et al.: J. Clin. Pharmacol., 45, 555 (2005)

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

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 Atorvastatin impurity. Atorvastatin Methyl Ester
References Graul, A., et al.: Drugs Future, 22, 956 (1997),

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 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 D
Applications 3-[4-(2-Methoxyethyl)phenoxy]-1,2-propanediol (Metoprolol EP Impurity D) is a new byproduct detected in Metoprolol tartrate. Metoprolol (M338790) impurity.
References Erickson, M., et al.: J. Pharmac. Biomed. Anal., 13, 567 (1995),

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

Impurity Atorvastatin EP Impurity G
Applications Atorvastatin derivative.

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 Telmisartan Acyl-β-D-glucuronide is a metabolite of Telmisartan (T017000).
References Abe, T., et al.: J. Biol. Chem., 274, 17159 (1999), Hirano, M., et al.: Drug Metab. Dispos., 34, 1229 (2006),

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 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 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);

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 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 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),

Applications A labelled inhibitor of glucose synthesis.
References Garcia-Salguero, L. et al.: Arch. Int. Physiol., Biochim. Biophys., 99, 237, (1991); Martirosyan, A., et al.: Biochem. Pharmacol., 68, 1729 (2004);

Applications Labelled 7α-Hydroxy-4-cholesten-3-one (H825130). 7α-Hydroxy-4-cholesten-3-one is a metabolite of Cholesterol (C432501).
References Connor, W., et al.: J, Clin. Invest., 48, 1363 (1969),

Applications (R)-Betaxolol is the R-isomer of Betaxolol (B328000), a cardioselective β1-adrenergic blocker (1,2,3). It is also an antihypertensive and antiglaucoma agent (4).
References (1) Bickel, M., et al.: J. Pharm. Pharmacol., 32, 669 (1980)(2) Cadigan, P.J., et al.: Br. J. Clin. Pharmacol., 9, 569 (1980) (3) Pathe, M., et al.: Therapie, 37, 75 (1982)(4) Panchal, V. S., et al.: J. Pharm. Sci. Pharmacol. 2, 21 (2015)

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),

Impurity Rosuvastatin EP Impurity C (Calcium Salt)
Stability Hygroscopic
Applications 5-Oxo Rosuvastatin (Rosuvastatin EP Impurity C (Calcium Salt)) is a Rosuvastatin (R700500) impurity.
References Endo, A., et al.: J. Antibiot., 32, 852 (1979), Beck, G., et al.: J. Med. Chem., 33, 52 (1990), Koga, T., et al.: Lipids, 30, 775 (1995),