Toxicology

Applications Stearoyl Ethanolamide is a prolific fatty acid ethanolamide produced by PLD hydrolysis of membrane phospholipids. Stearoyl Ethanolamide is also used for studying the effect on endocannabinoid signalling and BBB integrity in systemic inflammation. References Kasatkina, L. A., et al.: Biochem. Pharmacol. 174, 113783 (2020)

Applications N-[(1S,2S)-2-Hydroxy-3-[(2-methylpropyl)[(4-nitrophenyl)sulfonyl]amino]-1-(phenylmethyl)propyl]carbamic acid 1,1-dimethylethyl ester is an impurity of Darunavir (D193500), a human immunodeficiency virus (HIV) protease inhibitor that is used to treat patients with drug-resistant HIV. References Babu, K., et al.: Pharm. Chem., 3, 389 (2011); Back, D., et al.: Antivir. Ther., 13, 1 (2007); Ghosh, A., et al.: Bioorg. Med. Chem., 15, 7576 (2007)

Applications Process impurity of Darunavir-d9 synthesis. It is a COVID19-related research product.

Applications (R)-(-)-2-Amino-1-propanol is used as a reagent in the synthesis of naphthyridinone integrase 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 Johns, B.A., et al.: Bioorg. Med. Chem. Lett., 24, 3104 (2014)

Applications Labelled active form of Bisacodyl. Cathartic. References Roth, W., et al.: Arzneim.-Forsch. Drug Res., 38, 570 (1988), Bradshaw, K., et al.: J. Pharm. Biomed. Anal., 13, 1355 (1995), Wald, A., et al.: J. Clin. Gastroenterol., 36, 386 (2003),

Applications A compound used potentially for the radioiodination of monoclonal antibodies. Used in Antibody labelling. References Garg, P.K., et al.: Appl. Radiat. Isot., 40, 6, 485 (1989), Garg, P.K., et al.: Nucl. Med. Biol., 20, 4, 379 (1993),

Applications Cyclopyrrolone member of a family of non-benzodiazepine GABAA receptor agonists. This is a controlled substance (depressant) in the US but not in Canada. Sedative, hypnotic. References Noble, S., et al.: Drugs, 55, 277 (1998), Musch, B., et al.: Int. J. Clin. Psychopharmacol., 5, 147 (1990),

Applications Derivative of Artemisinin. Antimalarial. References Zhao, Y., et al.: J. Nat. Prod., 49, 139 (1986), Lin, A.J., et al.: J. Med. Chem., 30, 2147 (1987), Price, R. N., et al.: Expert Opin. Invest. Drugs, 9, 1815 (2000),

Applications 3-Bromopropionic-2,2,3,3-d4 Acid is the labeled analog of 3-Bromopropionic acid (B687705). 3-Bromopropionic Acid is used as a reagent in the synthesis of nitrogen containing diselenides which exhibit antioxidant activity. Also used as a reagent in the synthesis of indolin-2-one-based multi-targeted receptor tyrosine kinase inhibitors as potential anticancer agents. References Nascimento, V., et al.: Eur. J. Med. Chem., 87, 131 (2014); Zhang, L., et al.: Eur. J. Med. Chem., 82, 139 (2014)

Applications 2-Chlorophenylboronic Acid used in the preparation of imidazo[1,2-a]pyridine amides which has tuberculostatic activity. References Kang, S., et al.: J. Med. Chem., 57, 5293 (2014);

Applications N-Acetylpiperazine-d4 is labelled N-Acetylpiperazine-d4 which was used to prepare (aryl)sulfanyltriazoles with HIV-1 non-nucleoside reverse transcriptase inhibiting activities. It was also used to synthesize diphenylpyrazolecarboxamides as heat shock protein chaperone inhibitors and anticancer agents. References Wang, Z., et al.: Bioorg. Med. Chem. Lett., 16, 4174 (2006); Brough, P., et al.: J. Med. Chem, 51, 196 (2008)

Impurity Miconazole EP Impurity D Applications Isoconazole Nitrate acts as an antibacterial in the local treatment of vaginitis; antifungal agent (1,2). References 1. Asikoglu, M. et al.: J. Pharm. Pharmacol. 1995 Sep;47(9):717-202. Marrero-Ponce, Y. et al.: Bioorg. Med. Chem. 2005 Apr 15;13(8):2881-99

Applications Crotonoyl chloride is an unsaturated acid chloride that is used as an acylation agent in synthetic chemistry. Crotonoyl chloride is also used as a reagent in the synthesis of (-)-Exiguolide, a 16-membered macrolide that is used as a fertilization inhibitor. 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 Arumugam, V., et al.: Tetrahedron Lett., 38, 6473 (1997); Han, X., et al.: Eur. J. Org. Chem., 2013 (1193 (2013); Rathke, M. & Sullivan, D.: Tetrahedron Lett., 14, 1297 (1973)

Applications (4-(3-Methylbutan-2-yl)phenyl)methanol is an intermediate used in the synthesis of 1-Desmethyl-2-methylpropyl Amorolfine (D292315), which is an analogue of Amorolfine Hydrochloride (A634170). Amorolfine hydrochloride is a salt of Amorolfine which is a morpholine antifungal drug. It is a topical solution for the treatment of toenail infections. References Rotta, I., et al.: JAMA Dermatol., 149, 341 (2013); Espinel-Ingroff, A., et al.: Antimicrob. Agents Ch., 26, 5 (1984)

Applications Δ2-Cefuroxime Methyl Ester is a potentially related compound in cephalosporin antibacterial compounds. References Miyouchi, M., et al.: J. Chem. Pharm. Bull., 38, 1906 (1990), Sugioka, T., et al.: Chem. Pharm. Bull., 38, 1998 (1990),

Impurity Lamivudine EP Impurity H Stability Hygroscopic Applications Lamivudine (R)-Sulfoxide (Lamivudine EP Impurity H) is a metabolite of Lamivudine (L172500); a potent nucleoside reverse transcriptase inhibitor and antiviral agent. Lamivudine has been used for treatment of chronic hepatitis B. References Morris, D.M., J. Pharm. Biomed. Anal., 12, 255 (1944); Nevens, B.F., et al.: Gastroenterology, 113, 1258 (1997); Perry, C.M., et al.: Drugs, 53, 657 (1977)

Applications Desmethoxyamino Hydroxy Gemifloxacin is an Gemifloxacin (G336000) impurity, Third generation fluorinated quinolone antibacterial. References Wise, R., et al.: J. Antimicrob. Chemother., 44, 679 (1999), Allen, A., et al.: Antimicrob. Agents Chemother., 44, 1604 (2000), Blondeau, B., et al.: Expert Opin. Pharmacother., 5, 1117 (2004)

Applications Methyl 1-((2-Benzyloxycarbonxyl)phenyl)-2,3,4-tri-O-acetyl-β-D-glucopyranuronate-d4 is an intermediate in the synthesis of the metabolites of Nitazoxanide (N490100), an anthelmintic (cestodes), antiprotozoal (cryptosporidium) agent. References Honma, K., et al.: Chem. Pharm. Bull., 24, 394 (1976), Dubreuil, L., et al.: Antimicrob. Agents Chemother., 40, 2266 (1996), Stockis, A., et al.: Int. J. Clin. Pharmacol. Ther., 34, 349 (1996),

Stability Light Sensitive Applications 6α-Chloro Testosterone is a derivative of Testosterone, the principal hormone of the testes, produced by the interstitial cells. Major circulating androgen; converted by 5α-reductase in androgen-dependent target tissues to 5α-dehydrotestosterone which is required for normal male sexual differentiation. Also converted by aromatization to Estradiol.Testerone is a controlled substance (anabolic steroid). Androgen.This compound is a contaminant of emerging concern (CECs). References McFarland, K., et al.: Science, 245, 494 (1989), Heckert, L., et al.: Mol. Endocrinol., 12, 1499 (1998), Themmen, A., et al.: Endocr. Rev. 21, 551 (2000), Kumar, R., et al.: Biol. Reprod., 65, 710 (2001),

Stability Moisture Sensitive Applications Ethyl Malonyl Chloride is used as a reagent in the synthesis of novel thiadiazoloacrylamide analogs as inhibitors of dengue-2 virus NS2B/NS3 protease. Ethyl Malonyl Chloride is also used as a reagent in the synthesis of quinolone-benzylpiperidine derivatives as acetylcholinesterase inhibitors and antioxidant hybrids for Alzheimer disease. 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 Liu, H., et al.: Bioorg. Med. Chem., 22, 6344 (2014); Pudlo, M., et al.: Bioorg. Med. Chem., 22, 2496 (2014)

Applications 4-Hydroxy Darunavir is a metabolite of Darunavir (D193500), a novel inhibitor of human immunodeficiency virus protease and used in the treatment of HIV infection. It is a COVID19-related research product. References Vermeir, M., et al.: Drug. Meta. Disp., 37, 809 (2009); 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 Labelled S-(-)-Form of Ofloxacin. An antibiotic used against gram-negative organisms. References Kato, M., et al.: Arzneim.-Forsch., 42, 365 (1992), North, D.S., et al.: Pharmacotherapy, 18, 915 (1998), Hwang, D.G., et al.: Br. J. Ophthalmol., 87, 1004 (2003),

Applications N-Methyldiethanolamine-13C,d3 Hydrochloride is isotopically labelled salt form of N-Methyldiethanolamine (M301625), which is used as a reagent in the synthesis of broad-spectrum antimicrobial polycarbonate hydrogels with fast degradability. It is also used as a reagent in the synthesis of dihydroxy quaternary ammonium salts with long chain alkyl bromides that can exhibit antibacterial and antifungal activity. References Pascual, A., et al.: Biomacromolecules, 16, 1169 (2015); Liu, W., et al.: Chem. Biol. Drug Des., 85, 91 (2015);

Applications Chloroprocaine Diydrochloride-d4 is the labelled analogue of Chloroprocaine Hydrochloride (C380265), a local anaesthetic compound showing similar effects to Lidocaine. References Culp, W. et al.: Local Reg. Anesthe., 1, 11 (2008);

Applications Isotope labelled o-Cresol is a compound used as a disinfectant and have also been used as antiseptic in surgery. 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 Razavi, S.M., et al.: Nat. Prod. Res., 26, 2148 (2012); Asadollahi-B. M., et al.: Environ. Toxicol. Pharmacol., 34, 826 (2012);