Toxicology

Applications N6-Cyclopropyl-9H-purine-2,6-diamine is an impurity of Abacavir Sulfate (A105000), a nucleoside reverse transcriptase inhibitor (1,2,3). References (1) Daluge, S.M., et al.: Antimicrob. Ag. Chemother., 41, 1082 (1997) (2) Foster, R.H., et al.: Drugs, 55, 729 (1998) (3) Staszewski, S., et al.: J. Am. Med. Assoc., 285, 1155 (2001)

Applications Isotope labelled Erythromycin (E649950), an antibiotic useful for the treatment of a number of bacterial infection, usually prescribed to patients with allergy to penicillin. References Koch, W.L., et al.: Anal. Profiles Drug Subs., 8, 157 (1979),

Applications Labelled Dapoxetine (D185700). Selective serotonin reuptake inhibitor (SSRI). References Feret, B., et al.: Formulary, 40, 227 (2005),

Applications A metabolite of Loperamide; a new and improved PET radiotracer for imaging P-gp function. 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 Rahman, A., et al.: Cancer Res., 54, 5543 (1994), Sai, Y., et al.: Xenobiotica, 30, 327 (2000), Eneroth, A., et al.: Eur. J. Pharm. Sci., 12, 205 (2001), Kim, K., et al.: Drug Metab. Dispos., 31, 1090 (2003), Kannan et al. Drug Metab. Dispos., 38, 917 (2010)

Applications tert-Butylethyne, is an organic building block used for the synthesis of various pharmaceutical compounds, such as Terbinafine Hydrochloride (T107500), which is a synthetic allylamine antifungal. 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 Hadi, V., et al.: Tetrahedron Letters, 50, 2370 (2009); Petranyi, G., et al.: Science, 224, 1239 (1984);

Applications 2-[[(4R)-4-[(7-chloro-4-quinolinyl)amino]pentyl]ethylamino]-ethanol is an antimalarial drug more commonly known as (R)-hydroxychloroquine. References The Canadian Hydroxychloroquine Study Group: N. Engl. J. Med., 324, 150 (1991).

Applications Isopentenyl Pyrophosphate Triammonium Salt-13C2 is labelled Isopentenyl Pyrophosphate Triammonium Salt (I821850) which is used for the preparation of antitumor agents phosphohalohydrins. References Dhe-Paganon, S., et al.: Biochem., 33, 13355 (1994), Tanaka, Y., et al.: Nature, 375 155 (1995), Wesch, D., et al.: Eur. J. Immunol., 27, 952 (1997),

Applications 3,4-Dimethoxybenzenesulfonyl Chloride is used in the synthesis of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors. 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 Rosatelli, E., et. al.: Bioorg. Med. Chem. Lett., 24, 3422 (2014)

Impurity Clotrimazole EP Impurity A Applications (2-Chlorophenyl)diphenylmethane (Clotrimazole EP Impurity A) is a triarylmethane with antiproliferative activity. (2-Chlorophenyl)diphenylmethane is a degradation product of the antifungal agent Clotrimazole (C587400). Clotrimazole Related Compound A References Suzuki, M. Iyak. Kenk., 23, 44 (1992); Hajkova, R. et al.: Talanta, 73, 483 (2007); Sabourin, L. et al.: Environ. Toxicol. Chem., 30, 582 (2011);

Impurity Terbinafine EP Impurity E Dihydrochloride Salt Applications A Terbinafine dimeric impurity of the antifungal agent Terbinafine (T107500), an orally active, antimycotic allylamine related to Naftifine. A specfic inhibitor of squalene epoxidase, a key enzyme in fungal ergosterol biosynthesis. Antifungal. Also an impurity of SF 86-327 an antimycotic agent (2). References 1. Petranyi G. et al.: Science. 1984 Jun 15;224(4654):1239-41. 2. Ryder, N et al.: Antimicrob Agents Chemother. 1985 Feb;27(2):252-6.

Applications 2-Iodo-4-(1-methylethyl)-6-(trifluoromethyl)pyrimidine is a pyrimidine compound, generally used in the synthesis of pharmaceutical compounds, it may be used in the synthesis of cycloindoles for the treatment of hepatitis C.

Applications (5R)-5-Hydroxy-3-oxo-6-(benzyloxy)-hexanoic Acid tert-Butyl Ester is used in the preparation of antifungal macrolide antibiotic (+)-Roxaticin, Phorboxazole B and Bryostatin 2. References Evans, D. et al.: J. Am. Chem. Soc., 125, 10899 (2003); Evans, D. et al.: J. Am. Chem. Soc., 122, 10033 (2000); Evans, D. et al.: J. Am. Chem. Soc., 121, 7540 (1999)

Applications Labelled metabolite of Caffeine (C080100). References Grant, D.M., et al.: Clin. Pharm. and Ther., 33, 591 (1983),

Stability Hygroscopic Applications Amifostine Thiol is a metabolite of Amifostine (A576810) which provides normal cells with selective protection against the toxic effects of cancer chemotherapy and radiation treatment. References Satge, J., et al.: Eur. J. Med. Chem., 24, 48 (1989); Geary, R.S., et al.: Biopharm. Drug Dispos., 12, 261 (1991); Brown, D.Q., et al. Pharmacol. Ther., 39, 159 (1988); Capizzi, R.L., et al.: Cancer, 72, 3495 (1993); Treskes, M., et al.: Cancer Chemother. Pharmacol., 33, 93 (1993)

Applications A labelled metabolite of Efavirenz (E425000) (secondary metabolism). References Gorski, J., et al.: Biochem. Pharmacol., 47, 1643 (1994), Desta, Z., et al.: J. Pharmacol. Exp. Ther., 285, 428 (1998), Langmann, P., et al.: Eur. J. Med. Res., 7, 309 (2002), Chang, T., et al.: Drug Metab. Dispos., 31, 7 (2003),

Applications Paritaprevir is a pharmaceutical drug that is used in the treatment of hepatitis C virus in patients with HCV genotype 1 infection. It inhibits an important viral phosphoprotein, NS5A, which is involved in viral replication, assembly, and secretion. References Feld, J.J., et al.: New Eng. J. Med., 370, 1594 (2014); Lawitz, E., et al.: J. Hepatol., 57, 24 (2012); Afdhal, N., et al.: New England J. Med., 370, 1889 (2014)

Applications Metabolite of Diclofenac. References Duffy, J.C., et al.: J. Pharm. Pharmacol., 48, 883 (1996), Oza, V., et al.: J. Med. Chem., 45, 321 (2002), Bajaj, S., et al.: Bioorg. Med. Chem., 12, 3695 (2004), Teffera, Y., et al.: Drug Metabolism Lett., 2, 35 (2008),

Applications 1,1-Dimethylethyl Ester [(1S,2S)-2-Hydroxy-3-[(2-methylpropyl)amino]-1-(phenylmethyl)propyl]carbamic Acid is an intermediate in the synthesis of 2-epi-Darunavir (D193530), which is a stereoisomer to Darunavir (D193500), a second generation HIV-1-protease inhibitor; structurally similar to amprenavir. Antiviral. References Rao, R.N., et. al.: J. Sep. Sci., 35, 2671 (2012); Koh, Y., et al.: Antimicrob. Agents Chemother., 47, 3123 (2003); Arasteh, K., et al.: AIDS, 19, 943 (2005); Surleraux, D.L.N.G., et al.: J. Med. Chem., 48, 1813 (2005)

Applications An anthelmintic (Nematodes). References Baeder, C., et al.: Experientia, 30, 753 (1974), Van der Put, E., et al.: J. Immunol., 173, 818 (2004), Frasca, D., et al.: J. Immunol., 175, 6633 (2005),

Applications N-Boc-L-proline is a useful synthetic intermediate. It is used to synthesize Daclatasvir (D101500) which nhibits the HCV protein NS5A. Daclatasvir (D101500) can be used as a drug candidate for the treatment of hepatitis C (HCV). References Gao, M., et al.: Nature, 465(7294), 96 (2010); Bell, T. W., Chem. Med. Chem., 5(10), 1663 (2010);

Applications A metabolite of Ofloxacin (O245750). References Okazaki O., et al.: Xenobiotica, 22, 439 (1992), Murakami, K., et al.: Drugs, 49, 331 (1995),

Stability Very Hygroscopic Applications Labelled Oseltamivir Acid (O700980). Oseltamivir Acid is a metabolite of Oseltamivir (O701000). It is a COVID19-related research product. References Oliyai, R., et al.: Pharm. Res., 15, 1300 (1998), Kim, C.U., et al.: Med. Chem. Res., 8, 392 (1998), Hayden, F.G., et al.: N. Engl. J. Med., 341, 1336 (1999), Treanor, J.J., et al.: J. Am. Med. Assoc., 283, 1016 (2000)

Applications 2-Butyl-2-(2,4-dichlorophenyl)oxirane is an impurity of Hexaconazole (H293555), a fungicide of the triazole class. Hexaconazole has a broad spectrum antifungal activity and is commonly used in the control of apple, coffee and peanut diseases. References Brown, M.C. et al.: Bright. Crop Prot. Conf. Pest. Dis., 1, 229 (1988); Gozzo, F. et al.: Pest. Biochem. Physiol., 40, 68 (1991)