Toxicologie

Applications rac-Deacetamide Linezolid Phthalimide is a possible intermediate of Linezolid (L466500) which 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 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.
References Tsiang M. et al.: Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097;

Applications α-[2-[Methyl(1-naphthalenylmethyl)amino]ethyl]-Benzenemethanol is an impurity of naftifine (N213100) an antifungal.
References Stuetz, A., et al.: Journal of Medicinal Chemistry, 29, 112 (1986)

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 Emtricitabine Tenofovir Disoproxil Dihydrochloride is a derivative of Emtricitabine (E525000). Emtricitabine is a reverse transcriptase inhibitor. It is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.
References FASEB J., 13, 1511 (1999), Molina, J.-M., et al.: J. InfecSchinazi, R.F., et al.: Antimicrob. Ag. Chemother., 36, 2423 (1992), Shockeor, J.P., et al.: Xenobioica, 26, 189 (1996), Feng, J.Y., et al.: . Dis., 182, 599 (2000)

Applications 2-(Ethyl-d3) Isonicotinamide is an intermediate in the synthesis of Ethionamide-d3 (E890422), a labelled antibacterial (tuberculostatic) agent.
References Banerjee, A., et al.: Science, 263, 227 (1994), Newton, G., et al.: J. Bacteriol., 178, 1990 (1996), Baulard, A., et al.: J. Biol. Chem., 275, 28326 (2000), Koledin, T., et al.: Arch. Microbiol., 178, 331 (2002), Cardoso, R., et al.: Antimicrob. Agents Chemother., 48, 3373 (2004),

Applications Sedative, hypnotic
References Wegner, F., et al.: J. Neurochem., 107, 1056 (2008), McDonald, L., ewt al.: Psychopharmacol., 197, 591 (2008), Wegner, F., et al.: Eur. J. Pharmacol., 580, 1 (2008),

Applications Tenofovir Disoproxil is a therapeutic option for nucleos(t)ide analog (NA)-experienced chronic hepatitis B (CHB) patients infected with hepatitis B virus (HBV). Also, it is an intermediate used in the synthesis of Tenofovir Disoproxil Dimer (T018515), which is a Tenofovir Disoproxil impurity.
References Huang, M., et al.: Clin. Drug Investig., 36, 471-478 (2016); Cheng, G., et al.: Chem. Res. Toxicol., 16, 145 (2003)

Applications A potential metabolite of Exemestane (E957000).
References Buzzetti, F., et al.: Steroids, 58, 527 (1993),

Applications 4-Acetamidobenzene-d4-sulfonyl Chloride is the deuterium labelled form of 4-(Acetylamino)benzenesulfonyl Chloride (A170950), which is a sulfanilamide derivative of Chitosan with antifungal properties.
References Tashiro, T., et al.: Bioorg. Med. Chem., 16, 8896 (2008); Alcalde, E., et al.: J. Med. Chem., 52, 675 (2009);

Applications Emtricitabine O-β-D-Glucuronide Sodium Salt is a metabolite of (-)-Emtricitabine (E525000).
References Schinazi, R.F., et al.: Antimicrob. Ag. Chemother., 36, 2423 (1992); Shockeor, J.P., et al.: Xenobioica, 26, 189 (1996); Feng, J.Y., et al.: FASEB J., 13, 1511 (1999); Molina, J.-M., et al.: J. Infec. Dis., 182, 599 (2000);

Stability Hygroscopic
Applications A metabolite of (-)-Emtricitabine (E525000).
References Paff, M. et al.; Antimicrob. Agents Ch. 38, 1230 (1994)

Applications Nodakenin (CAS# 495-31-8) is a useful research chemical compound.

Applications N2-Methyl Trimethoprim-D3 is a labelled analogue of N2-Methyl Trimethoprim (M331190).

Impurity Clarithromycin EP Impurity E
Applications 6,11-Di-O-methyl Erythromycin (Clarithromycin EP Impurity E) is a Di-O-alkyl Erythromycin (E649950) is an impurity of Clarithromycin (C559750). Clarithromycin impurity E per British Pharmacopoeia.
References Morimoto, S. et al.: J. Antibiot., 43, 286 (1990); Kohno, Y. et al.: J. Antimicrob. Chemother., 26, 503 (1990);

Applications CMPD101 is a potent and selective GRK2/3 inhibitor.
References Lowe, J.D., et al.: Mol. Pharmacol., 88, 347 (2015); Ikeda, S., et al.: PCT Int. Appl. WO 2007034846 A1 20070329. Mar 29, 2007

Applications Dealkyl Fluticasone Furoate is a Fluticasone Furoate(F599510) raw material impurity which is a synthetic corticosteroid derived from fluticasone for treatment of seasonal allergic rhinitis.
References DeWester, J., et al.: Allergy Asthma Proc., 24, 331 (2003), Hughes, S., et al.: Drug Metab. Dispos., 36, 2337 (2008), Meltzer, E., et al.: Clin. Drug Investig., 29, 79 (2009),

Applications N-(3-Aminopropyl)-N-methylcarbamic Acid tert-Butyl Ester Hydrochloride is used as a reactant in the synthesis of 8-((dimethylamino)methyl)-1-(3-(dimethylamino)propyl)-1,7,8,9-tetrahydrochromeno[5,6-d]imidazol-2-amine, an inhibitor of the hepatitis C virus.
References Dirov, S.M., et. al.: J. Chem. Crystallogr., 43, 235 (2013)

Applications Chloroethylnitrosourea derivative with antitumor activity. Similar to carmustine, chlorozotocin, nimustine, ranimustine. Antineoplastic.
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 Johnston, T.P., et al.: J. Med. Chem., 9, 892 (1966), Oliverio, V.T., et al.: Cancer Res., 30, 1330 (1970), Thompson, G.R., et al.: Toxicol. Appl. Pharmacol., 21, 405 (1972), Al-Shammary, F.J., et al.: Anal. Profiles Drug Subs., 19, 315 (1990),

Applications 4'-[(4,5-Dimethyl-3-isoxazolyl)sulfamoyl]acetanilide is an renal metabolite of Sulfatroxazole (S699265), is an component present in various veterinary drugs.
References Nouws, J. F. M., et al.: J. Vet. Pharmacol. Ther., 12, 50 (1989);

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

Applications (±)-Napropamide-d10 (N,N-diethyl-d10) is a useful isotopically labeled compound of Napropamid (N378700)

Applications Cefdaloxime is an orally administered cephalosporin that has activity against Haemophilus influenzae, a bacteria that causes meningitis in humans. Cefdaloxime is also the active metabolite of HR916K, a cephalosporin ester.
References Jones, R. & Erwin, M.: Diag. Micro. Infect. Dis., 15, 693 (1992); Jones, R. & Erwin, M.: J. Clin. Micro., 30, 1297 (1992); Käyhty, R., et al.: J. Infect. Dis., 147, 1100 (1983)

Applications 14,15-Epoxy-moxidectin is a by-product during the synthesis of 3,4-Epoxy-moxidectin (E589045), which is derived from the parent compound Moxidectin (M744800), a macrocyclic lactone and semisynthetic derivative of nemadectin. Moxidectin is a parasiticide used for the prevention and control of heartworm and intestinal worms. Moxidectin is found in veterinary medicine used to treat animals such as dogs, cats, horses, cattle and sheep.Also, it is one of the impurities of Moxidectin under stress conditions.
References Bisset, S.A. et al.: New Zeal. Vet. J., 40, 97 (1992); Monahan, C.M. et al.: Vet. Parasitol., 63, 225 (1996); Glickman, L.T. et al.: Int. J. Appl. Res. Vet. Med., 3, 49 (2005); Awasthi, A., et al.: Anal. Bioanal. Chem., 404, 2203-2222 (2012)

Applications Desoxymycin is a derivative of streptomycin(S687223) which is an antibiotic produced by aerobic fermentation. Antibacterial (tuberculostatic).
References Weiss, et al.: Antibiot. Chemother., 7, 374 (1957), Umezawa, et al.: J. Antibiot., 27, 997 (1974), Mossa, J., et al.: Anal. Profiles Drug Subs., 16, 507 (1986),

Stability Hygroscopic, Moisture Sensitive
Applications 1-​[1-​(4-​Chlorobenzoyl)​-​5-​hydroxy-​2-​methyl-​1H-​indole-​3-​acetate]β-​D-​Glucopyranuronic Acid is an analog of Indomethacin Acyl-β-D-glucuronide a metabolite of Indomethacin (I641000). Acyl glucuronides have been implicated in the toxicity of many xenobiotics and marketed drugs.
References Abid, A., et al.: Biochem. Pharmacol., 50, 557 (1995), Gamage, N., et al.: Toxicol. Sci., 90, 5 (2006), Cerveny, L., et al.: Drug Metab. Dispos., 35, 1032 (2007), Hayeshi, R., et al.: Eur. J. Pharm. Sci., 35, 383 (2008),

Applications 6-Chloropurine 2'-Deoxy-Beta-D-ribofuranoside Diacetate is an intermediate in the synthesis of anti-hepatitis C virus agents.
References Patil, V.M., et. al.: Lett. Drug Des. Discov., 7, 139 (2010)

Applications MRX-2843, is an orally available small-molecule inhibitor of both MERTK and FLT3.
References Minson, K. A. et al.: JCI Insight. 2016 Mar;1(3):e85630.;

Applications Labelled Bexarotene (B336750). Used as an antineoplastic. A selective retinoid X receptor (RXR) agonist.
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)

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.
References Hoee, G., et al.: Pure Appl. Chem., 71, 11, 2019 (1999), Giannakakou, P., et al.: Proc. Natl. Acad. Sci. USA, 97, 2904 (2000)

Applications Labelled Phencyclidine (P295500). Anesthetic (intravenous). Controlled substance (depressant).
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 Chen, G., et al.: J. Pharmacol. Exp. Ther., 127, 241 (1959), Bailey, K., et al.: J. Pharm. Pharmacol., 28, 713 (1976), Balster, R.L., J. Psychedelic Drugs., 10115 (1978), Johnson, K.M., et al.: Annu. Rev. Pharmacol. Toxicol., 30, 707 (1990),

Applications 4-[4-(4-Methyloxy-phenyl)-piperazin-1-yl]-phenylamine, is an intermediate for the synthesis of Itraconazole (I937500), an Antifungal.