Toxicologie

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.
References McIntyre, J. A., et al.: Drugs. Future., 28, 859 (2003); LaMontagne, M.P., et al.: J. Medn. Chem., 32, 1728 (1989);

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

Applications A neuronal nicotinic acetylcholine receptor agonist. A CNS stimulant.
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 Damaj, M.I., et al.: J. Pharmacol. Exp. Ther., 282, 410 (1997), Toth, P.T., et al.: Eur. J. Pharmacol., 363, 75 (1998), Flammia, D., et al.: J. Med. Chem., 42, 3726 (1999), Dwoskin, P.A., et al.: Biochem. Pharmacol., 63, 89 (2002),

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.
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 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);

Applications Ritonavir O-Sulfate is a metabolite of Ritonavir (R535000); a selective HIV protease inhibitor. It is a COVID19-related research product.
References Daluge, S., et al.: Antimicrob. Agents Chemother., 38, 1590 (1994); Ammaranond, P., et al.: J. Clin. Virol., 26, 153 (2003), Harrigan, P., et al.: J. Infect. Dis., 191, 339 (2005); Miller, J., et al.: Bioorg. Med. Chem. Lett., 16, 1788(2006); Denissen, J.F., et al.: Drug Metab. Dispos., 25, 489 (1997)

Stability Temperature Sensitive
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.
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),

Applications Flavokavain B is a secondary metabolite of the kava plant (Piper methysticum Forst. f., Piperaceae, which has anticancer properties and demonstrated oral efficacy in murine cancer models.  Futhermore, it also has suspected roles in rare cases of kava-induced hepatotoxicity. In addition, it is a potential candidate for the development of novel antifungal phytotherapic products.
References Pinner, K. D., et al.: Pharmaceutical Biology (Abingdon, United Kingdom), 54, Epub ahead of print (2016); Rowe A., et al.: Phytotherapy Research, 26, 1768 (2012); Alves dos Santos, R., et al.: Journal of Chemistry, (2013)

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
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),

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

Applications Vinblastine-d3 Methiodide is the labeled analogue of Vinblastine Methiodide (V314015), an adduct of Vinblastine (V314000), an antitumor alkaloid isolated from periwinkle, Vinca rosea Linn., Apocynaceae; inhibits microtubule assembly. An antineoplastic.
References Dorman, D.E., Paschal, J.W.: Org. Magnetic Resonance, 8, 413 (1976); Lu, C., et al.: Cancer Research, 39, 3575 (1979); Gobbi, P.G., et al.: J. Clin. Oncol., 14, 527 (1996); Muhtadi, F.J., et al.: Anal. Profiles Drug Subs. Excip., 21, 611 (1992)

Applications Lorcainide Hydrochloride is an inhibitor of sodium voltage-gated channels. Effective anti-arrhythmic agents in patients.
References Lynch, J. J., et al.: J. Pharm. Exp. Ther., 273, 554-560 (1995); Heykants, J.: Int. Congr. Symp., 49, 35-39 (1981)

Applications Cilostazol-d4 is the labeled analogue of Cilostazol (C441500), a potent phosphodiesterase III A (PDE3A) inhibitor (IC50=0.2uM) and inhibitor of adenosine uptake. Has antimitogeni, antithrombotic, vasodilatory and cardiotonic properties in vivo. Also affects lipid levels in vivo.
References Suri, A., et al.: J. Clin. Pharmacol., 38, 144 (1998); Park, S.-W., et al.: Am. J. Cardiol., 84, 511 (1999); Tsuchikane, E., et al.: Circulation, 100, 21 (1999)

Applications Labelled Fenthion Sulfone (F278015). Fenthion Sulfone is a metabolite of the organothiophosphate insecticide Fenthion (F278000).
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 Oh, C., et al.: Bull Environ. Contam. Toxicol., 78, 314 (2007); Wang, W., et al.: Anal. Chim. Acta, 602, 211 (2007);

Applications A labelled deschloro analogue of the selective dopamine uptake inhibior Bupropion (B689625) with antidepressant-like activity.
References Foley, K. et al.: Drug Dev. Res., 60, 252 (2003);

Applications Cefpodoxime Proxetil-d7 is the labelled form of Cefpodoxime Proxetil (C243860), an antibacterial. Cefpodoxime Proxetil is a broad spectrum, orally absorbed third generation cephalosporin, ester prodrug of the active free acid metabolite, Cefpodoxime (C243850).
References Fujimoto, K., et al.: J. Antibiot., 40, 370 (1987), Utsui, Y., et al.: Antimicrob. Agents Chemother., 31, 1085 (1987),

Applications (S)-Benzylphenobarbital is a derivative of Phenobarbital (P316760), which is an Anticonvulsant; sedative; hypnotic.
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),

Applications Phorate Oxon is a toxic metabolite of Phorate (P353500), an inhibitor of acetylcholinesterase and pseudocholinesterase.
References Bowman, M.C. et al.: J. Agric. Food Chem., 17, 138 (1969); Hong, J.U. et al.: Han’guk Nong. Hakh., 26, 104 (1983); Szeto, S. et al.: J. Agric. Food Chem., 30, 1082 (1982);

Stability Hygroscopic
Applications A metabolite of Methylphenidate. Ethylphenidate is formed by metabolic transesterification of Methylphenidate and ethanol.
References Boyer, C., et al.: J. Pharmacol. Exp. Ther., 260, 939 (1992), Markowitz, J., et al.: Drug Metab. Dispos., 28, 620 (2000), Patrick, K., et al.: J. Med. Chem., 48, 2876 (2005),

Applications (3S,5S)-Dihydroxy Simvastatin is a derivtive of Simvastatin (S485000). Simvastatin is a synthetic derivative of a fermentation product of Aspergillus terreus. A competitive inhibitor of HMG-CoA reductase. A synthetic analog of Lovastatin. Antilipemic. Simvastatin, the drug, is sold under the trade name Zocor.
References Hoffman, W.F., et al.: J. Med. Chem., 29, 849 (1986), Mol, M.J., et al.: Lancet, 2, 936 (1986)

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

Applications An intermediate for the prepararion of 1-Hydroxypyrene β-D-Glucuronide, a metabolite of 1-Hydroxypyrene.

Stability Moisture Sensitive
Applications Sebuthylazine-d5 (ethyl-d5) (CAS# 1219805-56-7) is a useful isotopically labeled research compound.

Applications Erythromycin Ethyl Succinate-13C,d3 is the deuterated form of Erythromycin Ethyl Succinate (E649985), which is a derivative of Erythromycin (E649950), an antibiotic.
References Koch, W.L., et al.: Anal. Profiles Drug Subs., 8, 157 (1979); Serisier, D. et al.: J. Am. Med. Assoc., 309, 1206 (2013);

Applications Dehydronaproxen is an analog of Naproxen (N377520), an anti-inflammatory, analgesic, antipyretic. A non-steroidal anti-inflammatory.
References Harrison, I.T., et al.: J. Med. Chem., 13, 203 (1970);

Applications N,N-Diethyl-3-(mesitylsulphonyl)-1H-1,2,4-triazole-1-carboximidamide (Cafenstrole) (cas# 125306-83-4) is a useful research chemical.

Applications (R)-8-Hydroxy-3-methyl-1,2,3,4-tetrahydrobenz[a]anthracene-7,12-dione (cas# 681001-30-9) is a compound useful in organic synthesis.

Stability Hygroscopic
Applications A drug used for the treatment of atrial fibrillation and atrial flutter in patients who have suffered cardiac arrhythmias.
References Singh, B., et al.: J. Cardiovas. Pharmacol., 52, 300 (2008), Hoy, S., et al.: Drugs, 69, 1647 (2009), Hohnloser, S., et al.: New Eng. J. Med., 360, 668 (2009),

Applications 7,11-Hexadecadien-1-yl Acetate is a pheromone which can be used to disrupt the mating patterns of cotton bollworms and hence control their populations. It is also a fatty acid component of the Akebia trifoliata seed.
References Chamberlain, D.J., et al.: Bul. of Entom. Res., 83(3), 335-43 (1993);Ouyang, Yuzhu, et al.: Shipin Kexue, 31(20), 322-324 (2010);

Applications Ethofumesate is a herbicide.

Impurity Cefuroxime Axetil EP Impurity A
Applications Δ2-Cefuroxime Axetil (Cefuroxime Axetil EP Impurity A) is an oral prodrug of Cefuroxime (C248060), an injectable second generation cephalosporin with an excellent antibacterial activity. This ester is applied in therapy as a mixture of the R and S diastereoisomers.
References Nguyen, N., et al.: Pharm. Res., 8, 893 (1991), Stoeckel, K., et al.: Antimicrob. Agents Chemother., 42, 2602 (1998), Scott, L., et al.: Drugs, 61, 1455 (2001),

Applications Artemether- 13C, d3, is the labeled analogue of Artemether (A777400), which is a derivative of Artemisinin (A777500). Antimalarial, used to treat strains of malaria which are multi-drug resistant.
References Hombhanje, F., et al.: Pharma., 3, 3581 (2010), Michael, O., et al.: Malaria J., 9, 335 (2010), Cesar, I., et al.: J. Pharm. Biomed. Anal., 54, 114 (2011),

Applications An Efavirenz (E425000) impurity.

Applications Daptomycin Impurity B1-1 is an impurity of Daptomycin (D193350), cyclic lipopeptide antibiotic derived from a fermentation product of Streptomyces roseosporus; disrupts plasma membrane function in gram-positive bacteria. Antibacterial.
References Allen, N.E., et al.: Antimicrob. Agents Chemother., 31, 1093 (1987), Tully, F.P., et al.: Expert Opin. Invest. Drugs, 8, 1223 (1999),

Applications A labelled metabolite of the antipsychotic drug Trifluoperazine (TFP). Also a labelled metabolite of Fluphenazine.
References Mahju, M., et al.: Biochem. Pharmacol., 18, 2701 (1969), Breyer, U., et al.: J. Pharm. Sci., 63, 1842 (1974), Schmalzing, G., et al.: Drug Metab. Disp., 5, 104 (1977), Schmalzing, G., et al.: Xenobiotica, 8, 45 (1978),

Applications Tetrabromobisphenol S Dimethyl Ether-d6 is the isotope labelled analog of Tetrabromobisphenol S Dimethyl Ether (T291115); a useful insecticide against house flies and sugar beet aphids. Also found in coating mixtures used for fireproofing of polyester fibers.
References Pisanenko, D. A., et al.: Vestn. Kievskogo Politekhnicheskogo Instituta Khimicheskoe Mashinostroenie i Tekhnologiya, 25, 79 (1988); Tomita, M., et al. Fireproofing of polyester fibers and their blends. Jpn. Kokai Tokkyo Koho. JP 54006996 A 19790119. Jan 19, 1979

Applications Labelled Isoproturon. Pre-and post-emergence herbicide for control of annual grasses and broad-leaved weeds. Herbicide.
References Fournier, J.-C., et al.: Chemosphere, 4, 207 (1975), Gonzales, P., et al.: Weed Res., 23, 39 (1983),

Applications A metabolite of Cevimeline (C283500).

Applications Endothall-3,4,4,5,5,6-d6 Monohydrate (CAS# 1276197-30-8) is a useful isotopically labeled research compound.

Applications A bioequivalent prodrug of the DNA topoisomerase II inhibitor Etoposide (E933750). Antineoplastic used in the treatment of a wide variety of hematological malignancies and solid tumors.
References Kaul, S. et al.: J. Clin. Pharmacol., 13, 2835 (1995); J. Pharmakin. Biopharmac., 24, 313 (1996); Brooks, D.J. et al.: Anti-Cancer Drugs, 6, 637 (1995);

Applications 9-(2-Hydroxypropyl)adenine-13C5 is an intermediate used in the synthesis of rac Tenofovir-13C5 (>90%) (T018501), which is he isotope labelled analog of Tenofovir (T018500); an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor. Also used as an anti-HIV agent and antiviral.
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)

Applications Shows antioxidant effects. Antiseptic.
References Wong, S., et al.: Clin. Chem., 33, 214 (1987), Daood, H., et al.: Food Chem., 55, 365 (1996), Zainol, M., et al.: Food Chem., 81, 575 (2003),

Applications Micafungin-d11 Sodium is the isotope labelled analog of Micafungin Sodium (M342350); an echinocandin antifungal drug which inhibits the synthesis of 1,3-β-D-glucan, an essential component of the fungal cell wall. Micafungin Sodium also represents a valuable treatment option for fungal infections.
References Chen, S.C. et al.: Drugs, 71, 11 (2011); Groll, A.H. et al.: Opin. Anti-Infect. Invest. Drugs, 2, 405 (2000); Tomishima, M. et al.: J. Antibiot., 52, 674 (1999)

Applications Palmitoyl-L-carnitine-d3 Hydrochloride is labelled Palmitoyl-L-carnitine Hydrochloride (P155050), a long-chain fatty ester of carnitine which is accumulated and released into the circulation, in fatty-acid oxidation defects. Pattern of Lauroyl-L-carnitine can be diagnostic for a number of ß-oxidation defects.
References 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)

Applications Synthetic thrombin inhibitor. Antithrombotic.
References Abiko, Y., et al.: Thromb. Res., 24, 285 (1981), Kikumoto, R., et al.: Biochemistry, 23, 85 (1984),

Applications Hecogenin Acetate, is a derivative of Hecogenin (H129945), which is a sapogenin present in the leaves of species from the Agave genus, possessing wide spectrum of pharmacology activities, such as having antinociceptive properties.
References Gama, K. B., et al.: J. Natural Prod., 76, 559 (2013);

Applications Chlorthiophos is an organophosphorus pesticide.
References Lan, M., et al.: Sepu, 36, 938 (2018); Abbas, M. S., et al.: Int. J. Env. Anal. Chem., 97, 1003 (2017)

Applications Bosentan Acetate is a mixed endothelin receptor antagonist. Used as a vasodilator. Antihypertensive.
References Clozel, M., et al.: J. Pharmacol. Exp. Ther., 270, 228 (1994), Gutsch, G., et al.: Cardiovasc. Drugs Ther., 10, 717 (1996), Weber, C., et al.: Clin Pharmacol. Ther., 60, 124 (1996), Krum, H., et al.: N. Engl. J. Med., 338, 784 (1998)

Applications Dabigatran Etexilate Propanoate is an impurity of Dabigatran Etexilate (D100140). Dabigatran Etexilate is a nonpeptide, direct thrombin inhibitor. Antithrombotic.
References Mangiafico, R. et al.: Curr. Med. Chem., 19, 4688 (2012); Hu, Z. et al.: Anal. Bioanal. Chem., 405, 1695 (2013);

Applications Metribuzin DK is a selective triazine herbicide used in the control of broadleaf weeds. Used in the protection of vegetable and fruit crops. Pesticide.
References Xie, Y. et al.: Microchem. J., 133, 468 (2017);