Toxicologie

<p>Applications 6-Methyl-4-oxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide is an intermediate of Dorzolamide Hydrochloride (D535100), a carbonic anhydrase inhibitor. Antiglaucoma agent.<br>References Jiang, X., et. al.: Yingyong Huagong, 36, 1215 (2007); Lippa, E.A., et al.: Ophthalmology, 98, 308 (1991); Wang, R.-F., et al.: Arch. Ophthalmol., 109, 1297 (1991); Whikehart, D., et al.: J. Ocul. Pharmacol., 7, 195 (1991); Sjoquist, B., et al.: Drug Metab. Dispos., 26, 745 (1998)<br></p>

<p>Applications A galactosylceramide derivative used in the treatment of influenza. PBS-57 has the ability to stimulate both a cell-mediated and humoral immune response. Co-administration of PBS-57 with a vaccine may be used in methods to stimulate one or more of a humoral immune response, a CD4+ T cell response, and a CD8+ cytotoxic T cell response.<br>References Liu, Y., et al.: J. Immunol. Methods, 312, 34 (2006), Kamijuku, H., et al.: Mucosal Immunology, 1, 208 (2008), Kopecky-Bromberg, S; Vaccine, 27, 3766 (2009),<br></p>

<p>Applications A novel metabolite of Phenazopyridine (P313751).<br>References Bailey, K., et al.: Drug Metab. Dispos., 11, 277 (1983), Thomas, B. H., et al.: J. Pharm. Sci., 79, 321 (1990), Thomas, B.H., et al.: Xenobiotica, 23, 99 (1993),<br></p>

<p>Applications Indomethacin Acyl-β-D-glucopyranuronic Acid Phenyl Ester is a compound useful in organic synthesis.<br></p>

<p>Applications 4-Mercaptobenzonitrile is a building block used as a reactant in the synthesis and in vitro anti-hepatitis B virus activities of some ethyl 6-bromo-5-hydroxy-1H-indole-3-carboxylates.<br>References Chai, H., et al.: Bioorg. Med. Chem., 14, 911 (2006);<br></p>

<p>Applications Androstenedione (A637550) analog, an aromatase inhibitor.<br>References Marsh, D.A., et al.: J. Med. Chem., 28, 788 (1985),<br></p>

<p>Applications Nimbin (N476280) derivative.<br>References Cohen, E., et al.: Life Sci., 58, 1075 (1996), Roy, A., et al.: Biol. Pharm. Bull., 29, 191 (2006),<br></p>

<p>Stability Light Sensitive<br>Applications A thiol reactive water soluble fluorescent dye.<br></p>

<p>Applications Precursor to the fungicide, Posaconazole.<br>References Heeres, J., et al.: J. Med. Chem. 27, 894 (1984), Wood, P., et al.: Drug Discov. Develop., 1, 34 (1998),<br></p>

<p>Applications 5,5-Dimethyl-2-[[(phenylacetyl)amino]methyl]-4-thiazolidinecarboxylic Acid-d5 is the isotope labelled analog of 5,5-Dimethyl-2-[[(phenylacetyl)amino]methyl]-4-thiazolidinecarboxylic Acid. 5,5-Dimethyl-2-[[(phenylacetyl)amino]methyl]-4-thiazolidinecarboxylic Acid is a degradation product of Penicillins.<br>References Kiener, P.A., et al.: Biochem. J., 169, 197 (1978), Hilder, E., et al.: Electrophoresis, 23, 414 (2002), Pajchel, G., et al.: J. Pharm. Biomed. Anal., 32, 59 (2003),<br></p>

<p>Applications Lopinavir N2,N5-(2,6-Xylyloxy)acetyl Impurity is an impurity of Lopinavir (L469480), which is a selective HIV protease inhibitor. An analogue of Ritonavir. Antiviral. It is a COVID19-related research product.<br>References Sham, H.L., et al.: Antimicrob. Ag. Chemother., 42, 3218 (1998), Kumar, G.N., et al.: Drug Metab. Dispos., 27, 86 (1999), Murphy, R.L., et al.: Antiviral Ther., 4, Suppl. 3, 85 (1999)<br></p>

<p>Applications Erythromycin Cyclocarbonate is a derivative of Erythromycin (E649950), an antibcterial agent working on the 50S ribosomal subunit.<br>References Champney, W. et al.: Curr. Microbiol., 38, 342 (1999); Koch, W.L., et al.: Anal. Profiles Drug Subs., 8, 157 (1979),<br></p>

<p>Applications A labeled derivative of Amoxicillin (A634235), a 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 O-Arachidonoyl ethanolamine hydrochloride is a partial agonist at CB1 receptor and a full agonist at CB2 receptor. O-Arachidonoyl ethanolamine hydrochloride can be isolated from constituent of human and rat brain. It can be used to prepare antimicrobial arachidonic acid derivative.<br>References Kvasenkov, O. I. RU 2171610 C2 20010810 (2001); Sharir, H., et al.: J Neuroimmune Pharmacol. 7, 856 (2012)<br></p>

<p>Applications Oleoyl-L-carnitine-d3 is labelled Oleoyl-L-carnitine (O526700, HCl salt), a long-chain fatty ester of carnitine which is accumulated and released into the circulation, in fatty-acid oxidation defects. Pattern of Oleoyl-L-carnitine can be diagnostic for a number of ß-oxidation defects.<br>References Adams, S., et al.: J. Nutrition, 139, 1073 (2009); Ventura, F., et al.: Clinica Chimica Acta, 281, 1 (1999); Pourfarzam, M., et al.: Clinical Chem,, 40, 2267 (1994); Schaefer, J., et al.: Pediatric Res., 37, 354 (1995)<br></p>

<p>Applications 2-(1-(Ethylsulfonyl)-3-(4-(7-(hydroxymethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile is an impurity of Baricitinib (B118690), which is a JAK1 and JAK2 inhibitor and has been studied as a promising treatment for rheumatoid arthritis.<br>References Rodgers, J., et. al.: PCT Int. Appl. 185 pp.Patent (2009), WO 2009114512 A1 20090917;Dasari, S., et. al.: Russ. J. Org., 55, 1569 (2019);<br></p>

<p>Applications Bis-clindamycinyl-(2,2-dimethyltetrahydro-3aH-[1,3]dioxolo[4,5-c]pyran) Phosphate is an intermediate used in the synthesis of Bis-clindamycinyl Phosphate (B419135), which is an impurity of Clindamycin (C580000), an antibiotic prepared from Lincomycin (L466200), used to treat various infections.<br>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);<br></p>

<p>Applications A phenylpyridine derivative used in the preparation of HIV protease inhibitors I and other pharmaceutical agents.<br>References De Goey, D.A. et al.: J. Med. Chem., 52, 2571 (2009); Engstrom, K. et al.: J. Org. Chem., 71, 5369 (2006);<br></p>

<p>Applications Deschloro-2-phenylthio-thiamethoxam is an impurity of thiamethoxam (T344180), which is a neonicotinoid insecticide. Reports show that when exposed to neonicotinid pesticides honeybees have probelms returnign home after foraging and bumblebee colonies grow poorly and produce fewer queens.<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 Oliver, J., et al.: J. Environ. Horticult., 28, 135 (2010), Ghosh, A., et al.: J. Entomol. Res., 34, 35 (2010), Chem. and Eng. News 90: 10 (2012)<br></p>

<p>Impurity Abacavir EP Impurity A<br>Applications ent-Abacavir (Abacavir EP Impurity A) is an enatiomer of Abacavir (A105000). Abacavir is a carbocyclic 2'-deoxyguanosine nucleoside reverse transcriptase inhibitor and an anti-HIV drug used to treat HIV infection (1). Intracellular enzymes convert Abacavir to its active form, carbovir-triphosphate (CBV-TP), which then selectively inhibits HIV reverse transcriptase by incorporating into viral DNA (2). Abacavir is metabolized in the liver by uridine diphosphate glucuronyltransferase and alcohol dehydrogenase resulting in inactive glucuronide and carboxylate metabolites, respectively.<br>References (1) Jackson, A., et al.: Antivir Ther. 17, 19 (2012) (2) Yuen, G. J., et al.: Clin Pharmacokinet. 47, 351 (2008)<br></p>

<p>Applications Ampicillin Desoxyazetidin-2-one can be used to develop HPLC methods that detect compounds or impurities related to ampicillin in bulk drug. Ampicillin Desoxyazetidin-2-one is a related compound of Ampicillin (A634300), a β-lactam antibiotic used for treating bacterial infection. Ampicillin interferes with cell wall synthesis in bacteria.<br>References Raju, Ch. B. V. N., et al.: Anal Chem : Ind J, 7, 354 (2008); Fisher, J. F., et al.: Chem. Rev. 105, 395 (2005); Sill, M. L., et al.: Antimicrob. Agents Chemother. 52, 1551 (2008); Ivashkiv, E., et al.: Anal. Profiles Drug Subs. 2, 1 (1973)<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 1-(2-Chlorophenyl)hydrazine Hyrochloride is the salt form of 1-(2-Chlorophenyl)hydrazine (C375525); a useful research reagent used in the preparation of halogen-substituted phenylhydrazine derivatives with antifungal properties.<br>References Usui, Y., et al.: Yakugaku Zasshi, 87, 43 (1967)<br></p>

<p>Applications A diruetic. An antihypertensive.<br>References Curry, C.L., et al.: Clin. Ther., 9, 47 (1986), Kiyingi, A., et al.: Lancet, 335, 29 (1990)<br></p>

<p>Applications Methyl 5-Methyl-3-phenyl-4-isoxazolecarboxylate-d5 is an intermediate in the synthesis of Oxacillin Sodium-d5 Salt (O758502); Isotope labelled Oxacillin Sodium Salt is a semi-synthetic antibiotic related to Penicillin. Antibacterial.<br>References Goldenthal, E.I., et al.: Toxicol. Appl. Pharmacol., 18, 185 (1971),<br></p>

<p>Applications 2-Hydroxy Carbamazepine β-D-Glucuronide is a metabolite of 2-Hydroxy Carbamazepine (H884100).<br></p>

<p>Applications A selective A2A adenosine receptor agonist in myocardial imaging.<br>References Palle, V.P., et al.: J. A. Drug Dev. Res., 50, 64 (2000), Gordi, T., et al.: J. Clin. Pharmacol., 47, 825 (2007), Zhao, G., et al.: J. Cardiovas. Pharmacol., 52, 467 (2008), Botvinick, E., et al.: J. Nuc. Med. Technol., 37, 14 (2009),<br></p>

<p>Stability Hygroscopic<br>Applications A labelled metabolite from endophytes of the medicinal plant Erythrina crista-galli.<br>References Stadler, M., et al.: Planta Med., 60, 128 (1994), Kopcke, B., et al.: Phytochemistry, 60, 709 (2002), Chu, M., et al.: J. Nat. Prod., 66, 1527 (2003), Weber, D., et al.: J. Antibiot., 57, 559 (2004),<br></p>

<p>Applications Labelled Eltenac (E507000). A nonsteroidal anti-inflammatory drug.<br>References Allen, A., et al.: Gut, 21, 249 (1980), Tobin, T., et al.: J. Vet. Pharmacol. Therap., 9, 1 (1986),<br></p>

<p>Applications Acifluorfen-2-amino is a reduction product of Acifluorfen (A795248), a herbicide. Acifluorfen-2-amino is usually the first product in the degradation of Acifluorfen.<br>References Gennari, Mara, et al.: J. of Agri. and Food Chem., 42(5), 1232-6 (1994);Gooch, A. et al.: Env. Toxicol. Chem., 36, 2227 (2017)<br></p>

<p>Applications (+)-Nebivolol (N387896) metabolite.<br></p>

<p>Applications Labelled Bexarotene (B336750). Used as an antineoplastic. A selective retinoid X receptor (RXR) agonist.<br>References Boehm, M.F., et al.: J. Med. Che., 37,2930 (1994), Gottardis, M.M., et al.: Cancer Res., 56, 5566 (1996), Mukherjee, R., et al.: Nature, 386, 407 (1997), Miller, V.A., et al.: J. Clin. Oncol., 15, 790 (1997)<br></p>