Toxicology

Applications Myristamidopropyl dimethylamine (MAPD), present as Aldox in Opti-Free Express Disinfecting Solution for contact lens care, was tested for its potential as a drug in treatment of Acanthamoeba keratitis. MAPD is an amidoamine compound that shows activity against Acanthamoeba as well as a variety of other causal agents of microbial keratitis. References Stehr-Green, J., et al.: Am. J. Ophthalmol., 107, 331 (1989), Schuster, F., et al.: Clin. Microbiol. Rev., 15, 342 (2002), Hughes, R., et al.: J. Antimicrob. Chemother., 51, 1415 (2003),

Applications A degradation product of Orlistat (O686500). References Stalder, H. et al.: Helv. Chim. Acta, 73, 1022 (1990);

Applications Betamethasone 6α-Bromo 17-Valerate is an impurity of Betamethasone (B327000), which is a glucocorticoid used as an anti-inflammatory agent. References Ferrante, M.G., et al.: Anal. Profiles Drug Subs., 6, 43 (1977), Li, A., et al.: Chem. Biol. Interact., 142, 7 (2002), Cruz-Monteagudo, M., et al.: Eur. J. Med. Chem., 40, 1030 (2005), Rothfuss, A., et al.: Chem. Res. Toxicol., 19, 1313 (2006),

Applications The main labelled metabolite of Sulfamethoxazole. References Altenburger, R., et al.: Environ. Toxicol. Chem., 19, 2341 (2000), Pascoe, R., et al.: Anal. Chem., 73, 6014 (2001), Zhaohua, H., et al.: Eur. J. Med. Chem., 36, 863 (2001),

Applications Avibactam (NXL104) is a novel β-lactamase inhibitor with a non-lactam structural scaffold. NXL104 irreversibly inhibits lactamase from Mycobacterium tuberculosis. References Iland, C., et al.: J. Pathol. Bacteriol., 58, 495 (1946), Flores, A., et al.: Microbiology, 151, 521 (2005), Livermore, D., et al.: J. Antimicrob. Chemother., 62, 1053 (2008), Tremblay, L., et al.: Biochemistry, 49, 9685 (2010),

Stability Light Sensitive Applications Desacetyl Rifaximin is an impurity of Rifaximin (R509500), a non-absorbable semisynthetic Rifamycin antibiotic. References Brufani, M., et al.: J. Antibiot., 37, 1611 (1984); Gillis, J.C., et al.: Drugs, 49, 467 (1995); Huang, D.B., et al.: J. Infection, 50, 97 (2005)

Applications A major metabolite of Lopinavir (L469480) . It is a COVID19-related research product. References Molla, A., et al.: J. Virology, 250, 255 (1998), Sham, H., et al.: Antimicrob. Agents Chemother., 42, 3218 (1998), Kumar, G., et al.: Drug Metab. Dispos., 27, 86 (1999),

Applications An antimalarial. References Natarajan, L., et al.: Arzneim.-Forsch., 22, 1230 (1972), Kracmer, J., et al.: Pharmazie, 29, 773 (1974), Ahmad, I., et al.: Anal. Profiles Drug Subs., 21, 43 (1992),

Impurity Azithromycin EP Impurity L Applications Azithromycin N-Oxide (Azithromycin EP Impurity L) is an Azithromycin (A927000) impurity. A degradation products of Azithromycin. References Anon., et al.: Pharmaeuropa, 13, 750 (2001),

Applications Serotonin is a monoamine neurotransmitter. References Kuraishi, Y., et al.: Biol. Pharm. Bull., 31, 2143 (2008); Morera, E., et al.: Bioorg. Med. Chem. Lett., 19, 6806 (2009); Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010);

Impurity Clindamycin HCl EP Impurity B Applications Clindamycin B (Clindamycin HCl EP Impurity B) is a minor impurity of Clindamycin (C580000) in bulk drug. References Duckworth, C., et al.: J. Antimicrob. Agents Chemother., 31, 581(1993), Orwa, J., et al.: J. Pharm. Biomed. Anal., 23, 771 (2000), Platzer, D., et al.: J. Pharm. Biomed. Anal., 41, 84 (2006),

Applications A metabolite of all-trans Retinoic acid (R250200). References Idres, N., et al.: Cancer Res., 61, 700 (2001), Taimi, M., et al.: J. Biol. Chem., 279, 77 (2004), Vermot, J., et al.: Science, 308, 563 (2005),

Applications Fluorinated quinolone antibacterial (topical). References Kurokawa, I., et al.: J. Am. Acad. Dermatol., 25, 674 (1991),

Applications 2,2,2-Trifluoroethyl Formate acts as a reagent for the preparation of HCV NS5B inhibitor MK-3281, an inhibitor of hepatitis C virus. 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 Colarusso, S., et al.: Synlett, 11, 1527 (2011)

Impurity Miconazole EP Impurity I Applications Miconazole Impurity I (Miconazole EP Impurity I), is the impurity of Miconazole (M342500), which is an imidazole antifungal agent, that is applied topically to the skin or to mucus membranes for the treatment of fungal infections. 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 N-Desacetyl-N,O-descarbonyl O-Acetyl Linezolid Dihydrochloride is the salt form of D288280. N-Desacetyl-N,O-descarbonyl O-Acetyl Linezolid is an impurity of Linezolid (L466500); an oxazolidinone antimicrobial that inhibits bacterial mRNA translation. References Brickner, S.J., et al.: J. Med. Chem., 39, 673 (1996); Ford, C.W., et al.: Antimicrob. Agents Chemother., 40, 1508 (1996); Rybak, M.J., et al.: Pharmacotherapy, 18, 456 (1998); Stevens, D.L., et al.: Clin. Infect. Dis., 34, 1481 (2002)

Applications Isotope labelled Aminoacetonitrile Hydrochloride (A580055), a useful synthetic intermediate. It is a reagent used to synthesize dipeptide nitriles as reversible and potent cathepsin S inhibitors. It can also used to prepare substituted cyclic ureas as possible HIV protease inhibitors. References Ward, Y., et al.: J. Med. Chem., 45, 5471 (2002); Wilkerson, W., et al.: J. Med. Chem., 40, 4079 (1997)

Applications A potent local anesthetic that is active even in acidic conditions. It is used (usually in combination with an antacid) for the relief of pain associated with peptic ulcer disease or esophagitis. References Detrain, M. et al.: Acta. Gastro-Enterol. Belg., 28, 360 (1965); Barbezat, G.O. et al.: Scand. J. Gastroenterol., 13, 321 (1978); Masuda, Y. et al.: Biochem. Pharmacol., 64, 677 (2002);

Applications Stereoisomer to Darunavir (D193500), a second generation HIV-1-protease inhibitor; structurally similar to amprenavir. Antiviral. This is a labeled analog. It is a COVID19-related research product. References 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 Hexahydrocurcumin is a reagent in the synthesis of Gingerenone A (G387500) which is an antifungal and antiparasitic diarylheptenone that is isolated from Zingiber officinale (more commonly known as ginger), a medicinal plant that is used to treat inflammation and musculoskeletal disorders. References Ali, B., et al.: Food Chem. Toxicol., 46, 409 (2008); Bordia, A., et al.: Prost. Leuk. Ess. Fat. Acids, 56, 379 (1997); Choi, W., et al.: J. Appl. Biomed., 11, 15 (2013); Riaz, T., et al.: Nat. Prod. Res., 24, 1131 (2010); Srivastava, K. & Mustava, T.: Med. Hypoth., 39, 342 (1992)

Applications (E)-6-Amino-2-hexenoic Acid is used in the preparation of anti-collagenase active agent.

Stability Hygroscopic Applications Ethanolamine-13C2 Hydrochloride is the labeled analogue of Ethanolamine (E676500), which is used in the preparation of various pharmaceutical compounds and inhibitors. Ethanolamine-13C2, is also a 13C-labeled lipid precursor, used for the detection of phospholipid metabolism and the synthesis of phosphatidylethanolamine in T47D human breast cancer cells. References Ronen, S. M., et al.: Magnetic Resonance Med., 25, 384 (1992); Lombardo, L. et al.: J. Med. Chem., 47, 6658 (2004); Egan, T.: J. Med. Chem., 43, 283 (2000);

Applications Meclofenamic Acid is anti-inflammatory. It is used as an antipyretic. 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 Juby, et al.: J. Med. Chem., 11, 111 (1968), Winder, et al.: J. Pharmacol. Exp. Ther., 148, 422 (1965), Rees, M.C.P., et al.: Lancet, 2, 541 (1988),

Applications β-Amyrin is used as a protein tyrosine phosphatase 1B inhibitor with potential treatment towards diabetes. Also used in the synthesis of HIV-1 integrase inhibitory compounds based upon plant extracts. References Zhang, Y. et al.: Bioorg, Med. Chem., 16, 8697 (2008); Tewtrakul, S. et al.: Phytother. Res., 17, 232 (2003);

Applications Atazanavir is a novel azapeptide HIV protease inhibitor (PI). Antiviral. References Palella, F.J. Jr., et al.: N. Engl. J. Med., 338(13), 853 (1998), Nolan, D., et al.: Drugs, 63(23), 2555 (2003), Musial, B.L., et al.: Am. J. Health Syst. Pharm., 61, 1365 (2004), Wood, R., et al.: J. Acquir. Immune Defic. Syndr., 36, 684 (2004),

Impurity Clindamycin Phosphate EP Impurity E Stability Hygroscopic Applications Clindamycin Hydrochloride (Clindamycin Phosphate EP Impurity E) is a semi-synthetic antibiotic prepared from Lincomycin. Antibacterial. References Birkenmeyer, R.D., et al.: J. Med. Chem., 13, 616 (1970); Oesterling, et al.: J. Pharm. Sci., 59, 63 (1970); Gray, J.E., et al.: Toxicol. Appl. Pharmacol., 21, 516 (1972); Brown, L.W., et al.: Anal. Profiles Drug Subs., 10, 75 (1981);

Applications Emamectin B1 Benzoate is a neurotoxic pesticidal compound. A potential anti-leukemia agent. Also applied in pesticidal screening and control techniques. 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 Li, H., et al.: Agr. Sci. Tech., 15, 1707 (2014); Tang, T., et al.: Zhiwu Baohu, 42, 222 (2016); Yun, X., et al.: Environ. Toxicol. Pharmacol., 52, 280 (2017)

Applications An intermediate for the synthesis of Atazanavir-d5 and the preparation of some peptide analogs. References Martin, J., et al.: Prog. Med. Chem., 32, 239 (1995), Jadhav, P., et al.: J. Med. Chem., 40, 181 (1997), Bold, G., et al.: J. Med. Chem., 41, 3387 (1998).

Applications D-Valinol is used as a reagent in the synthesis of the HIV type 1 integrase inhibitor Elvitegravir (E509000). D-Valinol is also used in the preparation of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally active GSK-3β inhibitors for Alzheimer's disease. References Radl, S., et al.: J. Heterocyclic Chem., no vol., no pp. (2015, ahead of print); Fukunaga, K., et al.: Bioorg. Med. Chem. Lett., 25, 1086 (2015)

Applications Chlormidazole Hydrochloride has antimicrobial activity against aerobic bacteria and Candida species in vitro. It also has antifungal activity and is used in the treatment of dermatomycosis. References Krasiejko, I., et al.: Polski Tygodnik Lekarski, 45, 91 (1990); Michalowski, R., et al.: Mater. Ses. Nauk., 76 (1979); Ramisz, A., et al.: Nowosci Weterynarii, 13 (1983)

Applications (3S,5R)-[(1H-1,2,4-Triazol-1-yl)-methyl-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl]methyl Isobutyrate is an impurity of Posaconazole (P689600); an orally active triazole antifungal. References Cacciapuoti, A., et al.: Antimicrob. Agents Chemother., 44, 2017 (2000); Herbrecht, R., et al.: Int. J. Clin. Pract., 58, 612 (2004); Panackal, A., et al.: J. Clin. Microbiol., 44, 1740 (2006)

Applications The monoester metabolite of the adefovir prodrug Adefovir Dipivoxil (A280465). References Shaw, J.-P. et al.: Drug Metab. Dispos., 25, 362 (1997); Annaert, P. et al.: Pharmac. res., 15, 1168 (1998); Annaert, P. et al.: J. Pharmac. Sci., 89, 1054 (2000);

Stability Hygroscopic Applications A reverse transcriptase inhibitor. It is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner. A nucleoside analog structurally related to Lamivudine (L172500). References Mellors, J., et al.: Science, 72, 1167 (1996), Reimann, K., et al.: J. Virol., 79, 8878 (2005), Rose, J., et al.: J. Biol. Chem., 280, 7413 (2005), Acierno, P., et al.: J. Immunol., 176, 5338 (2006),