Toxicology

<p>Applications Isotope labelled Deschloro Ticlopidine is an impurity of Ticlopidine (T438325), an antithrombotic. A platelet aggregation inhibitor.<br>References Leblonde, G., et al.: Biochem. Pharmacol., 27, 2099 (1978), O’Brien, J.R., et al: Thromb. Res., 13, 245 (1978), Katsumura, T., et al.: Angiology, 33, 357 (1982),<br></p>

<p>Applications Chlorpropham is particularly useful in agricultural settings. It is used in pesticide products for treatment of plants and soil.<br>References Wozniak, E., et al.: PCT Int. Appl. (2020), WO 2020118278 A1<br></p>

<p>Stability Light Sensitive<br>Applications Metabolite of the immunosuppressant macrolide SDZ RAD (also known as Everolimus E945400) which is an analog of the parent drug Rapamycin (R124000).<br>References Vidal, C. et al.: J. Am. Soc. Mass Spec., 9, 1267 (1998); Kovarik, J. M., et al.: Clin. Pharmacol. Ther., 69, 48 (2001);<br></p>

<p>Applications Cefotaxime Sodium Impurity G-d3 is the isotope labelled analog of Cefotaxime Sodium Impurity G (C242955); an impurity of Cefotaxime Sodium (C242950) which is a broad spectrum third generation cephalosporin antibiotic.<br>References Wise, R., et al.: Antimicrob. Agents Chemother., 14, 807 (1978); Muhtadi, F.J., et al.: Anal. Profiles Drug Subs., 11, 139 (1982)<br></p>

<p>Applications Useful as vasodilators, antihypertensives, and spasmolytics.<br></p>

<p>Applications 1-Cyclopropyl-8-ethoxy-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic Acid is an impurity in the synthesis of Moxifloxacin (M745000), a fluorinated quinolone antibacterial.<br>References Woodcock, J.M., et al.: Antimicrob. Ag. Chemother., 41, 101 (1997), Stass, H., et al.: Antimicrob. Ag. Chemother., 42, 2060 (1998)<br></p>

<p>Applications Demethyltrichlorfon Sodium Salt is a metabolite of Trichlorfon (T773855), an irreversible organophosophate insecticide with acetylcholinesterase inhibitor activity and the prodrug of Dichlorvos (D435950).<br>References Najafi, N.M., et. al.: J. Struct. Chem., 52, 713 (2011); Li, R., et al.: App. Microbiol. Biotechnol., 94, 1553 (2012); Bakirci, G.T., et al.: Food. Chem., 135, 1901 (2012);<br></p>

<p>Applications Methyl 2-((((Benzyloxy)carbonyl)amino)methyl)-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxylate is an intermediate used in the synthesis of N-((5-Hydroxy-6-oxo-4-((2,4,6-trifluorobenzyl)carbamoyl)-1,6-dihydropyrimidin-2-yl)methyl)-1,3,4-oxadiazole-2-carboxamide (H950690), which is a derivative of Raltegravir (R100305), a potent integrase (IN) inhibitor for WT and S217Q PFV IN.<br>References Hare, S., et al.: Proc. Natl. Acad. Sci. U. S. A., 107, 20057 (2010); Hicks, C., et al.: Clin. Infect. Dis., 48, 931 (2009); Moss, D., et al.: Antimicrob. Agents Chemother., 56, 3020 (2012); Hare, S., et al.: Mol. Pharmacol., 80, 565 (2011)<br></p>

<p>Applications Labelled Oxycodone. Controlled substance (opiate). Analgesic (narcotic).<br>References Mendelson, J., et al.: Clin. Pharmacol. Ther., 60, 105 (1996), Fudala, P., et al.: N. Engl. J. Med., 349, 949 (2003), Alho, H., et al.: Drug Alcohol Depend., 88, 75 (2007),<br></p>

<p>Applications A labelled imidazole, a versatile heterocycle used in the preparation of various biologically active compounds such as the amino acid histidine and is present in many antifungal medication. It is also used extensively as a corrosion inhibitor on transition metals such as copper.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Arispe, N. et al.: Biophys. J., 95, 4879 (2008); Troesken, E.R. et al.: Endo. Res., 30, 387 (2004); Otmacic Curkovic, H. et al.: Corr. Sci., 51, 2342 (2009);<br></p>

<p>Applications Labelled analogue of Cyhexatin, a derivative of tricyclohexyltin and an effective acaricide used in the control of spider mites.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Jeppson, L.R. et al.: J. Econ. Entomol., 61, 1502 (1968); Rudd, J.A. et al.: Exp. Appl. Acarol., 21, 615 (1997);<br></p>

<p>Applications 1-(2,2-Dihydroxyethyl)-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic Acid is an intermediate in the synthesis of Bictegravir-15N, d2 (B382096), which is the labeled version of Bictegravir, which is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.<br>References Tsiang M. et al.: Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097;<br></p>

<p>Applications 17α-Testosterone-16,16,17-d3 Cypionate is the isotope labelled analog of 17α-Testosterone Cypionate (T155155); the 17α-isomer of Testosterone Cypionate (T155100) which is an anabolic steroid with androgenic properties. Also used for testosterone therapy in males with hypogonadism.<br>References Rabkin, J.G. et al.: J. Clin. Psychopharmacol., 19, 19 (1999); Hajjar, R. et al.: J. Clin. Endocrinol. Metab., 82, 3793 (1997); Rhoden, E. et al.: J. Sex Med., 7, 277 (2010)<br></p>

<p>Applications Vinclozolin is an agricultural fungicide which acts through an anti-androgenic mode of action, however is incapable of disrupting endocrine homeostasis (1). Affects male reproductive organs through increased gonad activity with spermatogenesis with deformities (2). Drinking water contaminant candidate list 3 (CCL 3) compound as per United States Environmental Protection Agency (EPA). Environmental contaminants; Food contaminants.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References 1. Flick, B. et al.: Arch. Toxicol. 2017 Apr;91(4):1941-1956.2. Watermann, B. et al.: J. Environ. Sci Health A Tox Hazard Subst Environ Eng. 2016 Nov 9;51(13):1111-20.<br></p>

<p>Applications 5-epi Emtricitabine Carboxylic Acid is an impurity of 5-epi Emtricitabine (E524980); an epimer of Emtricitabine (E525000) which is a nucleoside reverse transcriptase inhibitor approved for treatment of HIV-1. Emtricitabine also has antagonistic activity against the hepatitis B virus.<br>References Jeong, L., et al.: J. Med. Chem., 36, 181 (1993); Lim, S. et al.: Arch. Intern. Med., 166, 49 (2006); Smith, K., et al.: AIDS, 23, 1547 (2009)<br></p>

<p>Applications An Estradiol (E888000) 17-monoester. Short-chain fatty acid esters have a higher binding potency to the estrogen receptor than long-chain fatty acid esters. Estradiol fatty acyl esters act as a storage form from which estradiol is released by enzymic hydrolysis.<br>References Rifici, V., et al.: Metabolism, 41, 1110 (1992), Larner, J., et al.: J. Biol. Chem., 268, 13893 (1993), Tikkanen, M., et al.: Biochem. Pharmacol., 60, 1 (2000),<br></p>

<p>Applications (E)-1,1'-[2-(2,4-Difluorophenyl)-1-propene-1,3-diyl]bis-1H-1,2,4-triazole is an impurity of Fluconazole (F421000), an antifungal.<br>References Richard, K. et al.: Antimicrob. Ag. Chemother., 27, 832 (1985),<br></p>

<p>Impurity Cefixime EP Impurity F<br>Applications Cefixime Ethyl Ester is an ester impurity of the third generation cephalosporin antibiotic, Cefixime (C242800).<br>References Bian, L. et al.: Yao. Fen. Zaz., 30, 872 (2010);<br></p>

<p>Applications (Z)-2'-Deschloro Luliconazole is a Luliconazole (L473770) impurity. Luliconazole is an azole antifungal drug.<br>References Uhida, K., et al.: J. Infect. Chemother., 10, 216 (2004); Niwano, ., et al.: Antimicro. Agents Chemother., 42, 967 (1998)<br></p>

<p>Applications Isotope labelled D-Cycloserine inhibits cell wall biosynthesis (D-Ala peptide bond formation). D-Cycloserine also prevents conversion of D-Ala to L-Ala. D-Cycloserine is an bacteriostatic. D-Cycloserine is an antibiotic against Gram-negative bacteria.<br>References Lamb., J.W., et al.: Anal. Profiles Drug Subs., 1, 53 (1972), Gentry-Weeks, C., et al.: J. Biol. Chem., 268, 7298 (1993), Alexander, F., et al.: Eur. J. Biochem., 219, 953 (1994), Auger, S., et al.: Biochimie, 87, 231 (2005),<br></p>

<p>Applications Arachidonoyl p-Nitroaniline is a nitroaniline probe for FAAH activity.<br></p>

<p>Applications Labelled semi-synthetic antibiotic related to Penicillin. Antibacterial.<br>References Brogden, R.N., et al.: Drugs, 18, 169 (1979), Bird, A.E., et al.: Anal. Profiles Drug Subs. Excip., 23, 1 (1994),<br></p>

<p>Applications Isotope labelled Aminoacetonitrile (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.<br>References Ward, Y., et al.: J. Med. Chem., 45, 5471 (2002); Wilkerson, W., et al.: J. Med. Chem., 40, 4079 (1997)<br></p>

<p>Applications MCPA methyl ester is a derivative of MCPA which is a herbicide.<br>References Elliott, B., et al.: Mutagenesis, 20, 3 (2005), Pfleeger, T., et al.; Environmental Toxicology and Chemistry 30, 455 (2010)<br></p>

<p>Applications 4-Biphenylyl Sulfate Potassium Salt is a derivative of 4-Phenylphenol (P336135). 4-Phenylphenol is a reagent used in the synthesis of pyrrolo[1,2-c]imidazole dione derivatives as selective serotonin 5-HT1A receptor agonists with antinociceptive activity.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Valhondo, M., et al.: J. Med. Chem., 56, 7851 (2013); Nichols, D., et al.: Chem. Rev., 108, 1614 (2008)<br></p>

<p>Applications 1- tert-Butyl-3-[4-phenoxy-2,5-di(propan-2 -yl)phenyl]thiourea is an isomer of Diafenthiuron (D310550), an insecticide.<br>References Delbeke, F., et al.: Entomophaga, 42, 349 (1997); Mezcua, M., et al.: Anal. Chem., 81, 913 (2009);<br></p>

<p>Impurity Ganciclovir EP Impurity C<br>Applications 2’-Monodehydroxy-2’-chloro Ganciclovir is an Impurity of Ganciclovir (G235000). 2’-Monodehydroxy-2’-chloro Ganciclovir is a sugar modified acyclic analogue of guanosine (G837900). Studies have shown 2’-Monodehydroxy-2’-chloro Ganciclovir has potential to exhibit virucidal activity. Iso mono chloro ganciclovir<br>References Martin, J.C., et al.: J. Med. Chem., 29, 1384 (1986);<br></p>

<p>Applications N-Desmethyl rac-14-epi-Dextromethorphan is an intermediate in the synthesis of rac-14-epi-Dextromethorphan (D299440), which is an analog of Dextromethorphan (D299445) which is an antitussive compound showing analgesic properties. Dextromethorphan is used in cough medication formulations.<br>References Church J. et al.: Can J Physiol Pharmacol., 67, 561 (1989); Carliss, R. et al.: Neurotoxicology., 28, 813 (2007)<br></p>

<p>Applications 1,4-Diaminobutane is an amino acid degradation product. Used in the preparation of hexahydropyrimidines as novel hepatitis C virus inhibitors. Also a reagent in the synthesis of antibacterial castor oil-based polyurethane membranes.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Hwang, J. et al.: Eur. J. Med. Chem., 70, 315 (2013); Yari, A. et al.: J. Biomed. Mat. Res., 102A, 84 (2014);<br></p>

<p>Applications A reactive metabolite of Lapatinib (L175800) which is associated with various drug toxicities. Lapatinib is metabolized mainly by P450 3A4 to form O- and N-dealkylated metabolites.<br>References He, K., et al.: Chem. Res. Toxicol., 11, 252 (1998), Rusnuk, D., et al.: Cancer Res., 61, 7196 (2001), Li, X., et al.: Drug Metab. Dispos., 37, 1242 (2009),<br></p>

<p>Applications 2-(Bromomethyl)-5-(trifluoromethyl)furan is an intermediate used to prepare tertiary sulfonamides as liver X receptor antagonists. It is also used to synthesize hydantoin based inhibitors of MMP13 with potential use in osteoarthritis.<br>References Zuercher, W., et al.: J. Med. Chem., 53, 3412 (2010); De Savi, C., et al.: Bioorg. Med. Chem. Lett., 23, 4705 (2013)<br></p>

<p>Applications 3-Methylphosphinicopropionic Acid-d3 Diethyl Ester is a derivative of 3-Methylphosphinicopropionic Acid-d3 Sodium Salt (M326162), a metabolite of Glufosinate (G596950). 3-Methylphosphinicopropionic Acid-d3 Diethyl Ester is used in the preparation of the naturally occurring amino acid, Phosphinothricin.<br>References Zeiss, H.: J. Org. Chem., 56, 1783 (1991)<br></p>