Toxicologie

<p>Applications 3-Chloro-5-(trifluoromethyl)pyridine-2-carboxylic acid<br></p>

<p>Applications 17α-Cyanomethyl-19-nortestosterone is a metabolite of Norethindrone (N676000), an progesteron used in combination with estrogen as contraceptive.<br>References Oettel, M., et al.: Pharmazie., 48, 541 (1993); Wong, T.C., et al.: J. Chem. Soc., Perk. Trans., 5, 765 (1988); Schubert, K., et al.: Org. Chem., 20, 143 (1985);<br></p>

<p>Applications A metabolite of Phenobarbital (P316760).<br>References Soine, W.H., et al.: Drug Metab. Dispos., 12, 792 (1984), Soine, W.H., et al.: J. Pharmac. Sci., 80, 99 (1991),<br></p>

<p>Applications Isotope labelled (2R)-3-Carboxy-2-[(9-carboxy-1-oxononyl)oxy]-N,N,N-trimethyl-1-propanaminium Inner Salt is a useful intermediate that is often used in the metabolic studies of insulin production in humans.<br>References Shah, S.H.; et al.: Diabetologia, 55, 321 (2012)<br></p>

<p>Applications Terbufos-d10 (O,O-diethyl-d10) (CAS# 1276197-42-2) is a useful isotopically labeled research compound.<br></p>

<p>Applications 2-Nonyn-1-ol is a Propargyl alcohol (P762550) derivative that is used as a reagent to synthesize Microcarpalide, a microfilament disrupting agent that is weakly cytotoxic to mammalian cells. 2-Nonyn-1-ol is also thought to have potential antifungal properties.<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 Gershon, H., et al.: J. Pharm. Sci., 73, 1840 (1984); Ratnayake, A., et al.: Org. Lett., 3, 3479 (2001); Tamao, K., et al.: Tetrahedron Lett., 29, 6955 (1988)<br></p>

<p>Applications SN-38 4-Deoxy-glucuronide is a byproduct formed during the preparation of SN-38 Glucuronide.<br></p>

<p>Stability Hygroscopic, Moisture Sensitive<br>Applications Phorate Sulfoxide is a metabolite of Phorate (85%, P353500) which is a non-biocumulative organophosphate used as an insecticide and acaricide. Phorate is an inhibitor of acetylcholinesterase and pseudocholinesterase.<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 Pandey, G.C. et al.: Ind. J. Comp. Anim. Physiol., 6, 1 (1988); Henderson, M.C. et al.: Biochem. Pharmacol., 68, 959 (2004); Peter, J.V. et al.: NeuroToxicology, 29, 335 (2008);<br></p>

<p>Applications N-Docosanoyl Taurine is found to activate multiple members of the transient receptor potential (TRP) family of calcium channels, including TRPV1 and TRPV4 which are expressed in kidney.<br>References Saghatelian, A., et al.: Biochem., 45, 9007-9015 (2006)<br></p>

<p>Applications N2-(1-Ethylpropyl)-4,5-dimethyl-3-nitro-1,2-benzenediamine is a metabolite of Pendimethalin (P221900), an herbicide used to control the spread of weedgrass.<br>References Haith, D., et al.: Environ. Sci. Technol., 44, 6496 (2010); Jabran, K., et al.: Int. J. Agric. Biol., 12, 335 (2010); Rahaman, S., et al.: Environ. Ecol., 28, 1 (2010); Smith, R.H., et al.: Chemosphere, 8, 855-61 (1979);<br></p>

<p>Applications Chloroneb is a fungicide that has selective activity against certain fungi (e.g. Mucor and Pythium fungi), and is most commonly used for cotton seedlings and bean plants.<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 Gutenmann, W. &amp; Lisk, D.: J. Agr. Food Chem., 17, 1008 (1969); Lyr, H. &amp; Werner, P.: Pest. Biochem. Phys., 18, 69 (1982); Rhodes, R., et al.: J. Agr. Food Chem., 19, 745 (1971)<br></p>

<p>Stability Hygroscopic<br>Applications Isotope labelled Tenofovir Disoproxil Fumarate, an acyclic phosphonate nucleotide analogue; reverse transcriptase inhibitor. Used as an anti-HIV agent. Antiviral.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997), Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007),<br></p>

<p>Applications 6-METHYL-5-PROPYL-4(1H)-PYRIMIDINONE (cas# 103980-68-3) is a useful research chemical.<br></p>

<p>Applications Protected Ribavirin.<br>References Bhagrath, M., et al.: Antivir. Chem. Chemother., 2, 265 (1991), Zhu, T., et al.: Bioorg. Med. Chem. Lett., 20, 5212 (2010),<br></p>

<p>Applications A Nicorandil (N398500) derivative<br></p>

<p>Applications Furamidine is a diphenylfuran compound belonging to an important class of antimicrobial and antiparasitic agents. Furamidine and its analogues also display antitumor activities and showed antiproliferative activities against various tumor cell lines.<br>References Lansiaux, A. et al.: Cancer Res., 62, 7219 (2002); Steck E.A. et al.: Exp. Parasitol., 52, 404 (1981); Balzarini, J. et al.: Incest. New Drugs, 1, 103 (1983);<br></p>

<p>Applications (S)-7,8-Dihydroxy Efavirenz is a metabolite of (S)-Efavirenz (E425000); a nonnucleoside HIV-1 reverse transcriptase inhibitor.<br>References Young, S. D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995); Deng, Y., et al.: J. Sep. Sci., 38, 1529 (2015)<br></p>

<p>Applications Eugenol-glucuronide is a metabolite of Eugenol (E938640) formed in isolated rat hepatocytes.<br>References Thompson, David C., et al.: Chemico-Bio. Inter., 77(2), 137-47 (1991)<br></p>

<p>Applications A metabolite of Quinine.<br>References Small, D.L., et al.: J. Chem. Med., 22, 1014 (1979), Guentert, T.W., et al.: Eur. J. Drug Metab. Pharmacokinet., 7, 31 (1982), Rakhir, A., et al.: J. Pharmacokinet. Biopharm., 12, 1 (1984), Christie, D.J., et al.: J. Lab. Clin. Med., 112, 92 (1988),<br></p>

<p>Applications Des-N-(methoxycarbonyl)-L-tert-leucine Bis-Boc Atazanavir is an intermediate for the synthesis of Atazanavir (A790051) and the preparation of some peptide analogs.<br>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);<br></p>

<p>Applications Linear Daptomycin Hydrochloride Salt is the hydrochloride salt of L466470, which is the open-conformation of Daptomycin (D193350), cyclic lipopeptide antibiotic derived from a fermentation product of Streptomyces roseosporus; disrupts plasma membrane function in gram-positive bacteria. Antibacterial. Daptomycin Impurity<br>References Allen, N.E., et al.: Antimicrob. Agents Chemother., 31, 1093 (1987), Tully, F.P., et al.: Expert Opin. Invest. Drugs, 8, 1223 (1999),<br></p>

<p>Applications N2-Acetyl Acyclovir Benzoate-d5 is the isotope labelled analog of N2-Acetyl Acyclovir Benzoate (A167975); a derivative of Acyclovir (A192400) which is an orally active acyclic nucleoside with inhibitory activity towards several herpes viruses. Also an antiviral.<br>References Collins, P., et al.: J. Antimicrob. Chemother., 5, 431 (1979); Matsumoto, H., et al.: Chem. Pharm. Bull., 36, 1153 (1988); Whitley, R.J., et al.: N. Engl. J. Med., 327, 782 (1992); Ashton, D.S., et al.: J. Chromatogr. A, 707, 367 (1995)<br></p>

<p>Applications 2-Nitromorphine is an intermediate in the synthesis of 3-O-(Codein-2-yl)morphine (C634500), an impurity of Codeine (C634075).<br>References Chatterjie, N., et al.: Syn. Commun., 9, 647 (1979);<br></p>

<p>Applications Agomelatine-d3 (acetamide-2,2,2-d3) (CAS# 1079389-38-0) is a useful isotopically labeled research compound.<br></p>

<p>Applications An inhibitor of 5-lipoxygenase, the initial enzyme in the biosynthesis of leukotrienes from Arachidonic Acid. Used as an antiasthmatic.<br>References Carter, G.W., et al.: J. Pharmacol. Exp. Ther., 256, 929 (1991), Weinblatt, M.E., et al.: J. Rheumatol., 19, 1537 (1992), McGill, K and Busse, W.W.: Lancet, 348, 519 (1996)<br></p>

<p>Applications Tatenoquine is a new 8-aminoquinoline with an improved therapeutic index and safety profile as compared to primaquine (P733500).Tafenoquine has the potential to become a widely used drug in the prevention and treatment of malaria infection and could replace some currently used drugs as resistant strains of Plasmodium species increase.<br>References McIntyre, J. A., et al.: Drugs. Future., 28, 859 (2003); LaMontagne, M.P., et al.: J. Medn. Chem., 32, 1728 (1989);<br></p>

<p>Applications Fluoronitrofen contains pesticidal utility.<br>References Zhang, Y., et.al.: PCT Int. Appl. WO 2019236274 A1, 63, (2019);<br></p>

<p>Applications β-Adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic.<br>References Garteiz, et al.: J. Pharmacol. Exp. Ther., 179, 354 (1971), Taylor, S.H., et al.: N. Engl. J. Med., 307, 1293 (1982),<br></p>

<p>Applications N-Ethoxycarbonyl Dabigatran Ethyl Ester is an impurity of Dabigatran (D100090), which is antithrombotic drug.<br>References Hauel, N., et al.: J. Med. Chem., 45, 1757 (2002); Mungall, D., et al.: Curr. Opin. Invest. Drugs, 3, 095 (2002); Stangier, J., et al.: J. Clin. Pharmacol., 45, 555 (2005);<br></p>

<p>Stability Temperature Sensitive<br>Applications It is used in efficient synthesis of 1β-O-acyl glucuronides via regioselective acylation of allyl or benzyl D-glucuronate.Αcyl glucuronides are known metabolites of important drugs.<br>References Kaspersen, F., et al.: Xenobiotica, 17, 1451 (1987), Ebner, T., et al.: Drug Metab. Dispos., 27, 1143 (1999), Shipkova, M., et al.: Ther. Drug Monit., 25, 1 (2003), Stachulski, A., et al.: J. Med. Chem., 49, 6931 (2006),<br></p>

<p>Applications An intermediate in the synthesis of Epothilones. Epothilones are polyketide natural products that inhibit cancer cells by a mechanism similar to paclitaxel, and also are effective against paclitaxel-resistant tumours. Epothilone D is in phase I clinical testing of in patients with advanced solid tumours. Epothilone D is a cytotoxic macrolide that stabilises malignant cells' microtubules and arrests mitosis, a characteristic it shares with other epothilones. They bind to the same hepatic sites as does paclitaxel (Taxol) in a 1:1 stoichiometric ratio of a, b-tubulin heterodimers.<br>References Hoee, G., et al.: Pure Appl. Chem., 71, 11, 2019 (1999), Giannakakou, P., et al.: Proc. Natl. Acad. Sci. USA, 97, 2904 (2000)<br></p>

<p>Applications Chlorphentermine is an anorectic agent. Chlorphentermine is the 4-chloro derivative of the better known appetite suppressant Phentermine (P318830). Chlorphentermine is structurally related to amphetamine but is a relatively weak stimulant with little abuse potential.<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 Gylys, J.A. et al.: J. Pharmacol. Exp. Therap., 137, 365 (1962); Jun, H.W. et al.: Can. J. Pharmac. Sci., 4, 27 (1969); Luellmann, H. et al.: J. Pharm. Pharmacol., 25, 239 (1973);<br></p>

<p>Applications Atazanavir-8-(N-methoxycarbonyl)-L-tert-leucine Ester is an impurity of the drug Atazanavir (A790051). Atazanavir is a novel azapeptide HIV protease inhibitor (PI). Antiviral. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). Newer research has been investigating the potential anticancer effects of atazanavir<br>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),<br></p>

<p>Applications Labelled Olmesartan Medoxomil (O550000). Olmesartan Medoxomil is an angiotensin II receptor antagonist. Olmesartan Medoxomil is used as an anti-hypertensive.<br>References Yanagisawa, H., et al.: J. Med. Chem., 39, 323 (1996), Puchler, K., et al.: J. Hypertens., 15, 1809 (1997),<br></p>

<p>Applications N2-Des(L-valinyl) N2-Formal Lopinavir 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 N-Hydroxyphenylglycyl Cefadroxil-d4 is the isotope labelled analog of N-Hydroxyphenylglycyl Cefadroxil. N-Hydroxyphenylglycyl Cefadroxil is a derivative of Cefadroxil (C235750), which is a semi-synthetic cephalosporin antibiotic.<br>References Muggleton, et al.: Antimicrob. Agents Chemother., 253 (1968), Marrelli, L.P., et al.: Anal. Profiles Drug Subs., 4, 21 (1975),<br></p>

<p>Applications Fluenetil is a fluenethyl acaricide.<br>References Johannsen, F. R., et al.: Comp. Gen. Pharmacol., 5, 101 (1974), Johannsen, F. R., et al.: J. Econ. Entomol., 67, 5 (1974)<br></p>

<p>Applications The R-enantiomer of Baclofen (B108000) metabolite.<br></p>

<p>Applications Bivalirudin 1-11 Fragment is an impurity of Bivalirudin, a direct thrombin inhibitor acting as an anticoagulant through inhibition of the enzyme thrombin.<br>References Bertrand, O. et al.: Am. J. Cardio., 110, 599 (2012); Patti, G. et al.: Am. J. Cardio., 110, 478 (2012)<br></p>

<p>Applications Rosuvastatin Methyl Ester is an impurity of Rosuvastatin (R700500) in the pharmaceutical dosage forms under forced degradation conditions.<br>References Lennernas, H., et al.: Clin. Pharmacokinet., 32, 403 (1997), Kivisto, K., et al.: Br. J. Clin. Pharmacol., 46, 49 (1998), Lan, K., et al.: J. Pharm. Biomed. Anal., 44, 540 (2007),<br></p>

<p>Impurity Beclomethasone Dipropionate EP Impurity I<br>Applications (16β)-16-Methyl-17,21-bis(1-oxopropoxy)pregna-1,4,9(11)-triene-3,20-dione (Beclomethasone Dipropionate EP Impurity I) is an impurity of Beclomethasone (B131000), a glucocorticoid. Used in chronic asthma and allergic rhinitis. Antiallergic, antiasthmatic (inhalant). Anti-inflammatory (topical).<br>References Malfitan, V.A., et al.: Clin. Ther., 4, 472 (1982), Rao, M., et al.: J. Asthma, 19, 21 (1982), Small, P., et al.: Ann. Allergy, 49, 127 (1982), Brogden, R.N., et al.: Drugs, 28, 99 (1984),<br></p>

<p>Applications (S)-Benzylphenobarbital is a derivative of Phenobarbital (P316760), which is an Anticonvulsant; sedative; hypnotic.<br>References Goldenthal, E.I., et al.: Toxicol. Appl. Pharmacol., 18, 185 (1971), Chao, M.K.C., et al.: Anal. Profiles Drug Subs., 7, 359 (1978),<br></p>

<p>Applications 17β-neriifolin could be considered a candidate for the treatment of hepatocellular carcinoma. It can also work as an inhibitor of hERG channel trafficking.<br>References Zhao, Q., et al.:Fitoterapia, 82, 735 (2011); Wang, L., et al.: J. Pharmacol. Exper. Ther., 320, 525 (2007)<br></p>

<p>Stability Hygroscopic<br>Applications Atorvastatin (A791750) impurity.<br>References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996);<br></p>

<p>Applications Cloticasone is an intermediate in the synthesis of Fluticasone Propionate.<br>References Meltzer, E.O., et al.: J. Allergy Clin. Immunol., 86, 221 (1990), Mitchison, H.C., et al.: Gut, 32, 260 (1991), Phillipps, G.H., et al.: J. Med. Chem., 37, 3717 (1994)<br></p>

<p>Applications Phenindione is a proton pump inhibitor and traditional nonsteroidal anti-inflammatory drug used for acute interstitial nephritis and acute kidney injury.<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 Leonard, C.E., et al.: Pharmacoepidemiol. Drug. Safety., 21, 1155 (2012); Moda, T.L., et al.: Bioorg. Med. Chem. Lett., 22, 2889 (2012); Dhareshwar, S.S., et al.: J. Pharma. Sci., 99, 2711 (2010);<br></p>

<p>Applications Rosoxacin has shown to have antibacterial activity against Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus pneumoniae.<br>References Koba, M., et. al.: J. Mol. Modeling, 16, 327 (2010)<br></p>

<p>Stability Moisture Sensitive<br>Applications Oxyfedrine acts as a vasodilator affecting the coronary base flow.<br>References Baraka, Y. et al.: J. Drug Res., 12, 161 (1980);<br></p>

<p>Applications Norapomorphine Glucuronidate is a metabolite of Amomorphine (A727500). Amomorphine is a dopamine (D1 and D2) receptor agonist. Emetic. Antiparkinsonian.<br>References Neumeyer, J.L., et al.: J. Pharm. Sci., 59, 1850 (1970), Ginos, J.Z., et al.: J. Med. Chem., 18, 1194 (1975), Muhtadi, F.J., et al.: Anal. Profiles Drug Subs., 20, 121 (1991),<br></p>

<p>Stability Light and temperature Sensitive<br>Applications A glucuronide metabolite of Fluoxetine (F597100) in humans.<br>References Lemberger, L., et al.: J. Clin. Psychiatry, 46, 14 (1985),<br></p>