Toxicologie

Stability Hygroscopic
Applications The hydrochloride salt of AZ 5104 (A795170), which is a derivative of AZD 9291 (A808075) and a selective EGFR inhibitor (epidermal growth factor receptor), used in the treatments of nonsmall-cell lung cancer (NSCLC).
References Finlay, M.R.V., et al.: J. Med. Chem., 57, 8249 (2014);

Applications Desmethyl Nafcillin Sodium Salt is derived from (+)-6-Aminopenicillanic Acid (A618895), which is the core structure in penicillins, obtained from the fermentation brew of the Penicillium mold. (+)-6-Aminopenicillanic Acid is used as the main starting block for the preparation of numerous semisynthetic penicillins.
References Zel'tser, I.Z. et al.: Gig. Truda Prof. Zabol., 5, 59 (1983); Hamilton-Miller, J.M.T.: Int. J. Antimicrob. Agents, 31, 189 (2008); Novikova, N.D. et al.: Mikol. Fitopatol., 7, 101 (1973)

Applications Sericic acid is an antioxidant, PDE4A inhibitor, antiinflammatory, antifungal, and antibacterial.

Applications Stavudine 5-O-β-Glucuronide is the O-glucuronide derivative of Stavudine (S685250); a reverse transcriptase inhibitor and antiviral.
References Mansuri, M.M., et al.: Antimicrob. Ag. Chemother., 34, 637 (1990); Cretton, E.M., et al.: Antimicrob. Ag. Chemother., 37, 1816 (1993); Browne, M.J., et al.: J. Infec. Dis., 167, 21 (1993)

Applications Triclosan (3',5',6'-d3) O-β-D-Glucuronide Sodium Salt is an isotope labelled compound of Triclosan O-β-D-Glucuronide Sodium Salt (T774260), a metabolite of Triclosan (T774250).
References Moss, T. et al.: Food Chem. Toxicol., 38, 361 (2000); Wu, J. et al.: Sepu, 27, 724 (2009);

Applications Propisochlor is an herbicide that is absorbed through the shoots of germinating plants.

Applications A dinitronaphthaloyl derivative as disinfectants and antiseptics.
References Brana, M., et al.: Anti-Cancer Drug Des., 8, 257 (1993), Griffin, B., et al.: Science, 281, 269 (1998), Huh, W., et al.: Nature, 425, 686 (2003),

Applications (2-Fosfomycinyl-1-(hydroxy)propyl)phosphonic Acid is an impurity of Fosfomycin (F727500); an antibiotic compound used in the treatment of urinary tract infections.
References Liu, H., et al.: Zhongguo Kangshengsu Zazhi, 36, 765 (2011); Goto, M., et al.: Antimicrob. Agents Chemother., 20, 393 (1981); Keating, G. et al.: Drugs, 73, 1951 (2013); Demir, T. et al.: Int. J. Infect. Dis., 17, e966 (2013)

Applications epi-Velpatasvir is an impurity of antivaral drug Velpatasvir (V116000), which is a HCV NS5A inhibitor used to treat Hepatitis C.
References Feld, J. J., et al.: N. Engl. J. Med. 373, 2599 (2015); Gane, E. J., et al.: Gastroenterol., 151, 448 (2016);

Applications 3-(2-Chloro-6-fluorophenyl)-5-methylisoxazole-4-carboxylic Acid Ethyl Ester is a derivative in the synthesis of Flucloxacillin (F419200), a new semisynthetic penicillin with broad spectrum of antibacterial activity.
References Macsari, I., et al.: Bioorg. Med. Chem. Lett., 21, 3871 (2011); Cui, Y., et al.: Curr. Sci., 89, 531 (2005);

Stability Hygroscopic
Applications 2-Chloroethoxy Roxithromycin is an impurity of Roxithromycin (R700850); a semisynthetic Erythromycin (E649950) derivative and antibacterial.
References Jones, R.N., et al.: Antimicrob. Agents Chemother., 24, 209 (1983); Barry, A.L., et al.: Eur. J. Clin. Microbiol., 5, 536 (1986); Grassi, C., et al.: Chemioterapia, 6, 41 (1987); Gasc, J.C., et al.: J. Antibiot., 44, 313 (1991);

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 A metabolite of Varenicline. Metabolite M5.
References Dow, J., et al.: Drug Metab. Dispos., 22, 738 (1994), Toide, K., et al.: Biochem. Pharmacol., 67, 1269 (2004), Coe, J., et al.: J. Med. Chem., 48, 3474 (2005), Doll, R., et al.: Br. J. Cancer, 92, 426 (2005),

Impurity Beclometasone Dipropionate EP Impurity C
Applications An impurity of Beclomethasone Dipropionate (B131030).

Applications 6-Methylmercaptopurine Riboside-d3 is the isotope labelled analog of 6-Methylmercaptopurine Riboside (M321035); a thiopurine prodrug used as potential treatment for patients with inflammatory bowel disease.
References Haglund, S., et al.: Therap. Drug. Monitor., 33, 200 (2011); Arendt, C.S., et al.: J. BIol. Chem., 285, 6024 (2010); Fotoohi, A.K., et al.: Biochem. Pharmacol., 72, 816 (2006)

Applications O-Desmethyl Methylphenidate Carboxylic Acid is a derivative of Methylphenidate Hydrochloride (M325880), controlled substance (stimulant). CNS stimulant. Methylphenidate Carboxylic Acid Hydrochloride is a 4:1 Mixture of R533105 (DL-erythro Ritalinic Acid Hydrochloride) and R533110 (DL-threo-Ritalinic Acid Hydrochloride)
References Greenblatt, E.N., et al.: J. Pharmacol. Exp. Ther., 131, 115 (1961), Padmanabhan, G.R., Anal. Profiles Drug Subs., 10, 473 (1981), Srinivas, N.R., et al.: Pharm. Res., 10, 14 (1993),

Applications N-Methyl-1,3,5-triazine-2,4-diamine Metformin is an impurity of Metformin (M258858), which is a useful research chemical. This impurity can be used to prepare pyrazolo[1,5-a]pyrimidin-7(4H)-ones as methionine adenosyltransferase 2A inhibitors to treat cancer. It can also be used to prepare pyrazolopyrimidinones as inhibitors of cellular metabolic processes.
References Konteatis, Z.D., et.al., PCT Int. Appl., 474,(2018); Konteatis, Z.D., et.al., U.S.Pat Appl.Publ., 289,(2018);

Applications 8-Chloro-6-(2-fluorophenyl)-3a,4,5,6-tetrahydro-1-methyl-3H-imidazo[1,5-a][1,4]benzodiazepine-d3 is an isotope labelled impurity of Midazolam (M343000), a drug used for the treatment of acute seizures and is also known to exhibit activities as an anticonvulsant, sedative, and hypnotic.
References Dundee, J. W., et al.: Drugs, 28, 519 (1984); Lahat, E., et al.: Br. Med. J., 321, 83 (2000);

Applications Prometon-d3 (methoxy-d3) (CAS# 1219803-43-6) is a useful isotopically labeled research compound.

Applications Analgesic.
References Haddad, P., et al.: Drugs, 62, 1649 (2002), Chiu, P., et al.: J. Pharmacol. Sci., 95, 311 (2004), Dubin, A., et al.: J. Biomol. Screen, 10, 168 (2005),

Applications Butyric Anhydride-3,3,3',3',4,4,4,4',4',4'-d10 (CAS# 1398065-70-7) is a useful isotopically labeled research compound.

Applications 6-Methyl-1,3,5-triazine-2,4(1H,3H)-dione is a metabolite of metsulfuron methyl that has been found in soil.
References Ye, Q., Sun, J., Wu, J.: Environ. Pollut., 126, 417 (2003)

Impurity Ampicillin EP Impurity C Sodium Salt;
Applications Ampicillin Diketopiperazine Sodium Salt (Mixture of Diastereomers), is a a metabolite and impurity of the semi-synthetic antibiotic Ampicillin (A634300).
References Suwanrumpha, S. et al.: Biomed. Environ. Mass Spec., 18, 983 (1989); Zhu, Y. et al.: J. Pharmac. Biomed. Anal., 14, 631 (1996); Haginaka, J. et al.: J. Pharm. Pharmacol., 39, 5 (1987);

Applications Didemethyldiuron acts as a reagent in the synthesis of hydatoin derivatives with anticonvulsant properties. Derivative of Diuron (D494415), a phenyl urea herbicide. Pre-emergent herbicide.
References Mahjabin; S. et al.: Pharm. Chem., 7, 100 (2015); Norsworthy, J., et al.: Weed Technol., 24, 64 (2010), Armenta, S., et al.: Anal. Bioanal., Chem., 397, 297 (2010), Neuwoehner, J., et al.: Aquatic Toxicol., 97, 58 (2010), Wong, J., et al.: J. Agric. Food Chem., 58, 5897 (2010),

Stability Hygroscopic
Applications 42-O-tert-Butyldimethylsilyloxyethyl Rapamycin is a useful synthetic intermediate in the synthesis of Everolimus (E945400); an immunosuppressant macrolide and analog of the parent drug Rapamycin (R124000). Everolimus inhibits cytokine-mediated lymphocyte proliferation.
References Dumont, F.J., et al.: Curr. Opin. Invest. Drugs, 2, 1220 (2001); Kovarik, J. M., et al.: Clin. Pharmacol. Ther., 69, 48 (2001); Nashan, B., et al.: Ther. Drug Monit., 24, 53 (2002); Venkata, S.P., et al.: PCT Int. Appl. WO 2012066502 A1 20120524. May 24, 2012

Applications An intermediate in the preparation of HIV-integrase inhibitors
References Itoh, F., et al.: Chem. Pharm. Bull., 43, 230 (1995), Summa, V., et al.: J. Med. Chem., 51, 5843 (2008),

Applications N-Acetyl Cefixime is the N-acetylated analogue and impurity of the third generation cephalosporin antibiotic, Cefixime (C242800).

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 Bis(tributyltin) Oxide is an organotin compound used as a fungicide and molluscicide, particularly in wood preservation. Bis(tributyltin) Oxide was used as an active component in marine antifouling paints but is not longer used due to its toxicity and is considered a severe marine pollutant.
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 Laughlin, R.B.J. et al.: Environ. Sci. Technol., 20, 884 (1988); Polster, M. et al.: Ces.-Slov. Hyg., 15, 243 (1970);

Applications 2,5-Dichloro-1,3-benzenedicarbonitrile is a metabolite of the fungicide 2,4,5,6-tetrachloroisophthalonitrile (TPN) in soil.
References Sato, K., et al.: Biol. Fert. Soils, 3, 205 (1987)

Applications Propineb-d3 is the labeled analog of Propineb (P771450), which is used as a fungicide.
References Sharma, I.M., et. al.: J. Mycology Plant Pathology, 44, 92 (2014); Gupta, R.C., et. al.: Pestology, 37, 43 (2013)

Applications N-Acetyl-S-phenyl-DL-cysteine-3,3-d2 is the deuterium labelled form of N-Acetyl-S-phenyl-DL-cysteine, which is used as a reactant in the preparation of potent HIV-1 protease inhibitors that use D-amino acids as P2/P3 ligands.
References Jungheim, L., et al.: J. Med. Chem., 39, 96 (1996);

Stability Moisture Sensitive
Applications Labelled Chlorpyrifos Oxon (C425320). Chlorpyrifos Oxon is a metabolite of Chlorpyrifos (C425300) in human.
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 Atterberry, T., et al.: Toxicol. Appl. Pharmacol., 147, 411 (1997), Karanth, S., et al.: Toxicol. Sci., 58, 282 (2000), Barter, Z., et al.: Drug Metab. Dispos., 36, 2405 (2008),

Stability Hygroscopic
Applications Papain is used in the induction of T helper type 2 (Th2) immunity in the genital mucosa. Papain-functionalized gold nanoparticles as heterogeneous biocatalyst for bioanalysis and biopharmaceuticals analysis. Also used in the elucidation of the anti-proliferative activity of bovine blood hydrolyzates towards cancer cells including, lymphoma, breast cancer, hepatocytes and epithelial colorectal adenocarcinoma cells in cultureBiochem/physiol ActionsA cysteine protease that cleaves peptide bonds of basic amino acids, leucine, or glycine.pH optimum 6.0-7.0Also hydrolyzes esters and amides.Papain papaya latex has antifungal activity against C. albicans. It is a cysteine protease that cleaves peptide bonds of basic amino acids, leucine, or glycine.. The pH optimum is 6.0-7.0. Papain hydrol
References Oh, J. E.,et al.: Proc. Natl. Acad. Sci. USA, 114, 1188 (2017); Liu, S., et al.: Analytica Chimica Acta, 963, 33 (2017); O'Sullivan, S. M., et al.: Int. J. Food Sci. Technol., 52, 1049 (2017)

Applications Ethyl 3-(4-bromo-2-chlorophenyl)-3-oxopropionate (CAS# 131994-22-4) is a useful research chemical compound.

Applications Riluzole N-β-D-Glucuronide is the glucuronide conjugate and metabolite of Riluzole (R510000), a neuroprotective agent.

Applications Artemether Succinate Dimer is a derivative compound of Artemisinin (A777500), an antimalarial.
References Klayman, D.L., et al.: Science, 228, 1049 (1985); Price, R.N., et al.: Expert Opin. Invest. Drugs, 9, 1815 (2000); Meshnick, S.R., et al.: Int. J., Parasitol., 32, 1655 (2002);

Applications N-Demethyl Erythromycin A-d7 is a labeled version of N-Demethyl Erythromycin A (D230930), which is a metabolite of Erythromycin (E649950).
References Rich, D.H., et al.: J. Med. Chem., 18, 1004 (1975), Itoh, Z,. et al.: Antimicrob. Agents Chemother., 26, 863 (1984), Omura, S., et al.: J. Antibiotics 38, 1631 (1985)

Applications (R)-Chloropheniramine is an intermediate used in the synthesis of (R)-(-)-Chlorpheniramine Maleate (C424306), which is the R-enantiomer of Chlorpheniramine (C424300). Antihistaminic.
References Ishida, M., et al.: Int. J. Pharm., 359, 46 (2008), Moreno, R., et al.: Biomed. Chromatog., 24, 774 (2010), Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010),

Applications [2R-[2α(S*),4β]]-4-[[(2,2-Dimethyl-1-oxopropoxy)methoxy]carbonyl]-α-[[(hexahydro-1H-azepin-1-yl)methylene]amino]-5,5-dimethyl-2-thiazolidineacetic Acid is an impurity of Pivmecillinam (P550700), an orally active prodrug of Amdinocillin (A576300), an broad spectrum penicillin antibiotic that binds specifically to penicillin binding protein 2.
References Ejim, L., et al.: Nature. Chem. Biol., 7, 348 (2011); Lees, G.M., et al.: Brit. J. Pharmacol., 73, 535 (1981);