Toxicology

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 The erythro isomers have been shown to exhibit very little therapeutic effect and contribute mainly to the toxic hypertensive effects of this drug.Controlled substance.
References Greenblatt, E.N., et al.: J. Pharmacol. Exp. Ther., 131, 115 (1961), Padmanabhan, G.R., et al.: Anal. Profiles Drug Subs., 10, 473 (1981), Kuczenski, R., et al.: J. Pharmacol. Exp. Ther., 296, 876 (2001), Pelham, W.E., et al.: J. Consult. Clin. Psychol., 61, 506 (1993), Srinivas, N.R., et al.: Pharm. Res., 10, 14 (1993),

Applications A metabolite of Norfloxacin (N681000).
References Uno, T., et al.: J. Med. Chem., 33, 2929 (1990),

Applications Labelled Cyclosporin A (C988901) derivative. An immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection.A group of nonpolar cyclic oligopeptides with immunosupppressant activity.
References van Wartburg, A., et al.: Prog. Med. Chem., 25, 1 (1988), Jorgensen, K.A., et al.: Scand. J. Imunol., 57, 93 (2003), Vollenbroeker, et al.: Transplant. Proc., 37, 1741 (2005)

Applications 7-Keto Dehydro Epiandrosterone is a metabolite of Dehydroepiandrosterone (DHEA) (D229585).
References Majewska, M., et al.: Brain Res., 526, 143 (1990), Charlton, M., et al.: J. Neurochem., 68, 121 (1997), Koob, G., et al.: Biochem. Pharmacol., 68, 1515 (2004);

Applications Labelled Androgen. It has been used as an androgenic agent. Controlled substance (anabolic steroid).
References Bichet, N., et al.: Toxicol. Appl. Pharmacol., 106, 509 (1990), Gustafson, D., et al.: Toxicol. Sci., 53, 245 (2000), Copple, B., et al.: Toxicol. Sci., 77, 172 (2004), Takashima, K., et al.: Life Sci., 78, 2787 (2006),

Applications Aripiprazole-d8 is a deuterated version of Aripiprazole (A771000), a selective dopamine D2-receptor antagonist with dopamine autoreceptor agonist activity.
References Canive, J.M., et al.: Psychopharmacol. Bull., 34, 101 (1998), Oshiro, Y., et al.: J. Med. Chem., 41, 658 (1998),

Stability Hygroscopic
Applications N-[2-(2,4-Dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]-formamide is an impurity of miconazole (M342500). Antifungal (topical).
References Godefroi, E.F., et al.: J. Med. Chem., 12, 784 (1969), Brugmans, et al.: Arch. Dermatol., 102, 428 (1970), Heel, R.C., et al.: Drugs, 19, 7 (1980),

Applications Oseltamivir Namino-fructosyl Conjugate is derived from Oseltamivir Phosphate (O701000), which is an orally active inhibitor of influenza virus neuraminidase; converted in vivo to the active acid metabolite. An antiviral drug. 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 Bedaquiline is a diarylquinoline derivative that acts as a mycobacterial inhibitor. Bedaquiline shows promise as potential drug in the treatment of tuberculosis.
References de Jonge M.R. et al.: Proteins, 67, 971 (2007); Diacon A.H. et al.: N. Eng. J. Med., 360, 2397 (2009);

Applications Intermediate in the preparation of D-threo-Methylphenidate (Ritalin)

Applications Labelled ester analog of Rapamycin.
References Raymond, E., et al.: J. Clin. Oncol., 22, 2336 (2004), Galanis, E., et al.: J. Clin. Oncol., 23, 5294 (2005)

Applications Androgen. It has been used as an androgenic agent. Controlled substance (anabolic steroid).
References Bichet, N., et al.: Toxicol. Appl. Pharmacol., 106, 509 (1990), Gustafson, D., et al.: Toxicol. Sci., 53, 245 (2000), Copple, B., et al.: Toxicol. Sci., 77, 172 (2004), Takashima, K., et al.: Life Sci., 78, 2787 (2006),

Applications is an isotopic labeled compound of Acetamiprid-N-desmethyl (C428803); an acetamipride-Metabolite that performs insecticidal and neuroblocking activities in animals.
References Kiriyama, K., et al.: J. Pest. Sci., 28, 17 (2003); Gbylik-S., et al.: J. Chromatogr. B: Analyt. Technol. Biomed. Life Sci., 990, 132 (2015)

Stability Store in freezer
Applications A caffeine metabolite.
References Regal, K.A., et al.: J. of Chromatography B, 708, 75 (1998)

Applications Tirofiban intermediate.

Applications A peripheral benzodiazepine GABAA receptor ligand, a new anxiolytic.
References Min, D., et al.: Pharmacotherapy, 12, 68 (1992), Rothwell, C., et al.: J. Toxicol. Sci., 27, 35 (2002), Gonzalez-Diaz, H., et al.: Bioorg. Med. Chem. Lett., 15, 1651 (2005), Boelsterli, U., et al.: Curr. Drug Metab., 7, 715 (2006), Rietjens, I., et al.: Chem. Res. Toxicol., 19, 977 (2006),

Applications A labelled metabolite of Theophylline.
References ottrup, A., et al.: Pharmacol. Toxicol., 67, 340 (1990), El-Kadi, A., et al.: Drug Metab. Dispos., 28, 1112 (2000), Kim, S., et al.: J. Med. Chem., 45, 2131 ( 2002), Hansel, T., et al.: Drugs Today, 40, 55 (2004),

Stability Hygroscopic, Moisture Sensitive
Applications Phoxim-d5 (Phenyl-d5) (Mixture of Isomers) is a useful isotopically labeled compound of Phoxim (P380000(P)), which is an organophosphate insecticide. Phoxim is also an analogous dimethyl ester and an organothiophosphate acaricide.
References Lu, Y., et al.: Nature, 487, 362 (2012); Jokanovic, M., et al.: Arch. Toxicol., 70, 119 (1995); Wang, W., et al.: Pest. Biochem. Physiol., 84, 180 (2006)

Applications Antibacterial.
References Manius, G.J., et al.: Anal. Profiles Drug Subs., 7, 445 (1978), Roth, B., et al.: J. Med. Chem., 23, 379 (1980), Brogden, R.N., et al.: Drugs, 23, 405 (1982),

Stability Hygroscopic
Applications Labelled Iopromide. Nonionic, injectable radio-contrast medium. Diagnostic aid (radiopaque medium).
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 Muetzel, W., et al.: Am.J. Neuroradiol., 4, 350 (1983), Dawson, P., et al.: Acta Radiol. Diagn., 25, 253 (1984),

Stability Hygroscopic
Applications Chlorhexidine Digluconate Impurity K was found in a study of the kinetics of chlorhexidine hydrolysis.
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 Zong, Z., Lee, E.K.: J. Pharm. Sci., 101, 2417 (2012)

Applications Testosterone ester. Testosterone 17-Valerate has been a useful compound in the development of immunochemical techniques for detection of anabolic androgenic steroids in food supplements.
References Ruelle, P., et al.: Int. J. Pharm., 157, 219 (1997), de la Torre, X., et al.: J. Pharm. Biomed. Anal., 24, 645 (2001), Adat, S., et al.: Lett. Drug Des. Discov., 1, 334 (2004), Holubova, B., et al.: Eur. Food Res. Technol., 245, 1011 (2019)

Applications Labelled Dimethomorph (D460530). Agricultural fungicide.
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 Lu, X., et al.: Phytopathol., 100, 1162 (2010), Schafer, R., et al.: Environ. Sci. Technol., 45, 1665 (2011),

Stability Hygroscopic
Applications Synthetic thrombin inhibitor. Thrombin mutant anticoagulant antagonist. Antithrombotic.
References Dewanjee, M., et al.: J. Nucl. Med., 22, 981 (1981), Goodman, S., et al.: J. Biomed. Mater. Res., 45, 240 (1999), Carlsson, S., et al.: Thromb. Res., 115, 9 (2005),

Impurity Clarithromycin EP Impurity I
Applications De(cladinosyl) Clarithromycin (Clarithromycin EP Impurity I) is an impurity of Clarithromycin (C559750). De(cladinosyl) Clarithromycin showed significantly potent antibacterial activity against community acquired respiratory pathogens.
References Morimoto, S., et al.: J. Antibiot., 37, 187 (1984), Buxbaum, A., et al.: J. Antimicrob. Chemother., 52, 371 (2003), Westphal, J., et al.: Br. J. Clin. Pharmacol., 50, 285 (2000), Ma, Z., et al.: J. Med. Chem., 44, 4137 (2001),

Applications Oligomycin A is a macrolide antibiotic with fungicidal activity isolated from Streptomyces species.
References Nakakita, Y. et al.: J. Antibiotics., 33, 514 (1980);

Applications Methoxyphenamine hydrochloride, is the salt version of methoxyphenamine (OMMA), a β-adrenergic receptor agonist, that regulates norephinephrine and ephinephrinein concentrations.
References Chahl, L.A. et al.: Brit. J. Pharmacol., 45, 510 (1972);

Stability Hygroscopic
Applications Oseltamivir 5-Desamino 5-(2-Formyl 5-Hydroxymethylpyrrol-1-yl) is derived from Oseltamivir Phosphate (O701000), which is an orally active inhibitor of influenza virus neuraminidase; converted in vivo to the active acid metabolite. An antiviral drug. 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 Novel intermediate of Azithromycin that acts as antibiotic.
References Krajacic, M.B., et al.: J. Antibiot., 58, 380 (2005),

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.
References Smith, S., et al.: Am. J. Cardiol., 80, 10H (1997), Jacobsen, W., et al.: Drug Metab. Dispos., 28, 1369 (2000), Istvan, E., et al.: Science, 292, 1160 (2001), Tabernero, L., et al.: J. Biol. Chem., 278, 19933 (2003), Bratton, L., et al.: Bioorg. Med. Chem., 15, 5576 (2007),

Applications Anabolic steroid. Controlled substance.
References Schneider, M., et al.: J. Biotechnol., 46, 161 (1996), Bao, S., et al.: Biol. Reprod., 62, 616 (2000), Imamura, T., et al.: J. Biol. Chem., 280, 20171 (2005),

Applications 7-Hydroxy-furo[3,4-b]pyrazin-5-one is a derivative of 6-(5-Chloro-2-pyridyl)-6,7-dihydro-7-hydroxy-5H-pyrrolo[3,4-b]pyrazin-5-one (C379925) which is an impurity of Eszopiclone (E889150), a nonbenzodiazepine hypnotic agent used as a treatment for insomnia.
References Gottesmann, C., et al.: Eur. J. Neurosci., 10, 409 (1998), Yoshimoto, M., et al.: Eur. Neuropsychopharmacol., 9, 29 (1999),

Impurity Cefotaxime Sodium EP Impurity E
Applications 3-Desacetyl Cefotaxime Lactone is an impurity of Cefotaxime sodium (C242950). 3-Desacetyl Cefotaxime Lactone is also a degradation product for other cephalosporin antibiotics such as: Ceftriaxone (C245000), Cefodizime and Ceftiofur (C244700).
References Amaker, R., et al.: Antimicrob. Agents Chemother., 40, 1139 (1996), Taylor, P., et al.: Clin. Biochem., 38, 328 (2005),

Applications Testosterone (T155000) derivative.
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),

Applications A potent inhibitor of taurine transport.
References Guidotti, A., et al.: Pharmacol. Res. Commun., 2, 341 (1970),

Impurity Itraconazole Impurity 16
Applications cis-[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-4-yl-methyl)-1,3-dioxolan-4-yl]methyl Methanesulfonate (Itraconazole Impurity 16) is an impurity in the synthesis of Itraconazole (I937500), an orally active antimycotic structurally related to Ketoconazole. Antifungal.
References Espinel-Ingroff, A., et al.: Antimicrob. Agents Chemother., 26, 5 (1984), Heykants, J., et al.: Mycoses, 32, Suppl 1, 67 (1989);