Toxicologie

Applications Primary alkaloid of various species of Cinchona (Rubiaceae). Optical isomer of Quinidine. Antimalarial; muscle relaxant (skeletal).
References Muhtadi, F.J., et al.: Anal. Profiles Drug Subs., 12, 547 (1983), Kremsner, P.G., et al.: J. Infect. Dis., 169, 467 (1994),

Impurity Clarithromycin EP Impurity F
Applications 12-O-Methyl Clarithromycin (Clarithromycin EP Impurity F) is a methylated impurity of the semi-synthetic macrolide antibiotic Clarithromycin (C559750). 12-O-Methyl Clarithromycin was shown to inhibit uptake of Clarithromycin into the lung cells.
References Chen, X. et al.: Zhong. Yao., 17, 32 (2008); Yoshida, H. et al.: Jap. J. Antibiot., 53, 615 (2000); Omura, S. et al.: Yakug. Zas., 112, 593 (1992);

Applications N,O-Bis(trimethylsilyl)acetamide is used as a reagent in the synthesis of 4'-spirocyclic phosphono-nucleosides as potential inhibitors of hepatitis C virus NS5B polymerase. Also used as a reagent in the microwave-assisted synthesis of purine nucleosides as selective cholinesterase inhibitors.
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 Dang, Q., et al.: Tetrahedron Lett., 55, 4407 (2014); Schwarz, S., et al.: Org. Biomol. Chem., 12, 2446 (2014)

Applications Used as an antibacterial agent. LD50 >5000 mg/kg for oral administration to rats.
References Goldenthal, E.I.: Toxicol. Appl. Pharmacol., 18, 185 (1971)

Impurity Ceftazidime EP Impurity A
Stability Hygroscopic, Light Sensitive
Applications ∆2-Ceftazidime, 90% (Ceftazidime EP Impurity A) is a Ceftazidime isomer, an impurity of Ceftazidime (C244100).
References Vilanova, B., et al.: Helv. Chim. Acta, 76, 2789 (1993), Zhou, M., et al.: J. Pharm. Sci., 84, 534 (1995), Baertschi, S., et al.: Chemother. 8, 353 (1997), Porra, R., et al.: J. Pharm. Biomed. Anal., 18, 241 (1998),

Applications 5-Chloro-2-furancarbonyl 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 Erythromycin Lactobionate is an antibiotic used to reduce the prevalence of drug resistant bacteria as well as keeping constant the efficacy of other antibacterial drugs.
References Kiso, S. et al.: Anticanc. Res., 20, 2827 (2000); Broad, J. et al.: Brit. J. Pharm., 168,1859 (2013); Itoh, Z., et al.: Antimicrob. Agents Chemother., 26, 863(1984)

Stability Hygroscopic
Applications Tenofovir Monohydrate is an HIV-1 RT inhibitor and antiretroviral drug.
References Zhao, Z., et al.: Method for preparing medical salts and/or derivatives of tenofovir disoproxil, and their application for preventing and/or treating HBV and HIV/AIDS infections, CN 101574356 (2009);

Applications Hydroxychloroquine O-Sulfate Sodium Salt is an analogue and potential metabolite of the antimalarial drug Hydroxychloroquine (H916900). Studies suggest that there is increased uptake and retention of Hydroxychloroquine O-Sulfate in blood of rheumatoid arthritis subjects. It is a COVID19-related research product.
References Lucherini, T. et al.: Recenti Prog. Med., 33, 446 (1962); Mueting, D.: Nature, 195, 1003 (1962);

Applications 2,2,4-Trimethyl-6(2H)-quinolinone 1-Oxide is a derivative of 2,6-Dihydro-2,2,4-trimethyl-6-quinolone (D449900) which is a metabolite of Ethoxyquin (E892800), an oxidation product of the antidegradant.
References Kahl, R., et al.: Toxicology, 28, 229 (1983), Burka, L., et al.: Xenobiotica, 26, 597 (1996), Bammler, T., et al.: Toxicol. Sci., 54, 30 (2000), Hayes, J., et al.: Cancer, 174, 103 (2001),

Applications Atazanavir is a novel azapeptide HIV protease inhibitor (PI). Antiviral.
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),

Stability Light Sensitive
Applications An intermediate in the preparation of Omeprazole metabolites.
References Hoffmann, K., et al.: Drug Metab. Disposition, 14, 341 (1986), Andersson, T., et al.: Brit. J. Clin. Pharmacol., 36, 521 (1993),

Applications Epitizide is a diuretic agent.
References Pilsbury, V., et al.: J. Pharm. Pharmacol., 18, 713 (1966), Tisdall, P., et al.: Clin. Chem., 26, 702 (1980),

Stability Too Hygroscopic
Applications Erdosteine Thioacid Diammonium Salt is the active metabolite of Erdosteine (E596050), a mucolytic. Erdosteine was developed for the treatment of chronic obstructive bronchitis.
References Dechant, K., et al.: Drugs, 52, 875 (1996); Braga, P., et al.: Arzneim.-Forsch., 49, 344 (1999); Braga, P., et al.: Antimicrob. Agents Chemother., 43, 1013 (1999); Kuvandik, G., et al.: Toxicol. Pathol., 36, 714 (2008); Koyu, A., et al.: Mol. Cell. Biochem., 331, 43 (2009); Fourches, D., et al.: Chem. Res. Toxicol., 23, 171 (2010)

Stability Hygroscopic
Applications Dipotassium Glycyrrhizinate is used in improving the dissolution property of amphotericin B (AMB) and the bioavailability of the drug incorporated in suppositories.
References Tanaka, M., et. al.: Chem. Pharm. Bull., 40, 1559 (1992);

Applications Mebutizide is a thiazide diuretic.
References Madrid A.J. et al.: Rev. Clin. Esp., 114, 143 (1969);

Applications Sulforaphene is an extract from the seeds of Raphanus sativus and displays anti-inflammatory and anti-cancer activity.
References Kim, K. et al.: J. Ethnopharmacol., 151, 503 (2014);

Applications Labelled Dodecyl Phthalate (D525380). Dodecyl Phthalate is used in the preparation of Cytarabine (C998100) derivatives as anticancer agents.
References Aoshima, M., et al.: Cancer Res., 36, 2726 (1976), Wang, N., et al.: Bioorg. Med. Chem. Lett., 15, 4064 (2005), Marie-Helene, G., et al.: Bioorg. Med. Chem., 2009, 17, 6340 (2009),

Applications n-Pentyl 4-Hydroxybenzoate-2,3,5,6-d4 (CAS# 1219798-66-9) is a useful isotopically labeled research compound.

Applications A metabolite of the fluorinated quinolone antibacterial Ciprofloxacin.

Applications 5,6-Dihydroyangonin is a derivative of Yangonin (Y100550), a lactone isolated from the Kava plant (Piper methysticum). 5,6-Dihydroyangonin was shown to exhibit potential antibacterial and antifungal activities.
References Keledjian, J., et al.: J. Pharm. Sci., 77, 1003 (1988), Clouatre, D., et al.: Toxicol. Lett., 150, 85 (2004), Mathews, J., et al.: Drug Metab. Dispos., 33, 1555 (2005), Clayton, N., et al.: Exp. Toxicol. Pathol., 58, 223 (2007),

Stability Hygroscopic
Applications Piperacillin sodium is an antibiotic related to penicillin. Also, it possesses anti-microbial activity against enterobacteria.
References Zhang, Y., et al.: Linchuang Wuzhen Wuzhi, 27, 63-65 (2014)

Impurity Sofosbuvir Metabolite GS331007
Applications RO 2433 is the deaminated metabolite of β-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine, an effective inhibitor of hepatitis C virus (HCV) replication in vitro.
References Asif, G., et. al.: Antimicrob. Agents Ch., 51, 2877 (2007)

Applications The S,S-stereoisomer of Chloramphenicol (C325030). Broad spectrum antibiotic obtained from cultures of the soil bacterium Streptomyces venezuelae. It has a broad spectrum of activity against Gram-positive and gram-negative bacteria. Antibacterial; antirickettsial.
References Bartz, et al.: J. Biol. Chem., et al.: 172, 445 (1948), Gottlieb, et al.: J. Bacteriol., 55, 409 (1948), Szulczewski, D., et al.: Anal. Profiles Drug Subs., 4, 47 (1975), Price, A., et al.: J. Antibiot., 43, 118 (1981), Shalit, I., et al.: Drugs, 28, 281 (1984),

Stability Hygroscopic
Applications Desacetyl Rifampicin Quinone is an impurity of Rifampicin (R508000).
References Wilson, W.L. et al.: J. Chrom., 144, 270 (1977);

Applications Efavirenz Pen-3-ene-1-yne is an analog of Efavirenz (E425000), a nonnucleoside HIV-1 reverse transcriptase inhibitor and antiviral agent.
References Young, S.D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995)

Applications N-Demethyl Rifampicin is a metabolite of Rifampicin (R508000).
References Marsili, L., et al.: J. Antibiot., 37, 1209 (1984), Nikaido, H., et al.: Antimicrob. Ag. Chemother., 37, 1393 (1993), Piddock, L., et al.: J. Antimicrob. Chemother., 45, 159 (2000),

Stability Hygroscopic
Applications 5R,6R-Benzylpenicilloic Acid is the β-lactamase cleavage product/metabolite of antibiotic Penicillin G (P223400).
References Dryjanski, M., Pratt, R.: Biochem., 34, 3561 (1995); Ho, H., et al.: Rapid Commun. Mass Spectrom., 25, 25 (2011);

Applications Terbinafine is used to treat infections caused by a fungus.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Applications Acriflavine is an topical antiseptic agent and has also been used for the treatment of external fungal infections. Dyes and metabolites.
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 Weisman, J.L., et al.: Chem. Biol. Drug. Des., 67, 409 (2006); Sala, C., et al.: Antimicro. Agents. Chemother., 54, 4150 (2010);

Applications Elaiophylin is a macrolide antibiotic with immunosuppresive activity.

Applications Apixaban-13C, d3 is labelled Apixaban (A726700) which is a potent, direct, selective, and orally active inhibitor of coagulation factor Xa. It is a potential new oral coagulant that may be useful prevention of venous thromboembolism in total hip, knee replacement orthopedic surgery and stroke in treatment of patient with venous thromboembolic disorder or with atrial fibrillation.
References Luettgen, J.M. et al.: J. Enz. Inhib. Med. Chem., 26, 514 (2011); Glanis, T. et al.: J. Thromb. Thrombol., 31, 310 (2011); barrett, Y.C. et al.: Thromb. Haemos., 105, 181 (2011);

Applications Labelled Talinolol. Selective β1-adrenergic blocker structurally related to Practolol. Antihypertensive; antiarrhythmic.
References Assmann, I., et al.: Curr. Med. Res. Opin., 13, 325 (1995), Trausch, B., et al.: Biopharm. Drug Dispos., 16, 403 (1995),

Applications Atorvastatin Calcium Salt Trihydrate is a compound used as standard in the method development and validation for simultaneous determination of Atorvastatin calcium (A791750) and Ezetimibe (E975000) in tablets using UV spectrophotometric, HPLC and HPTLC methods.
References Rajamanickam, V., et al.: World Appl. Sci. J., 9, 1424-1429 (2010);

Applications Used as a reference standard for the drug Trimethoprim.Note this compound is a cis / trans mixture.

Applications An antimalarial.
References Natarajan, L., et al.: Arzneim.-Forsch., 22, 1230 (1972), Kracmer, J., et al.: Pharmazie, 29, 773 (1974), Ahmad, I., et al.: Anal. Profiles Drug Subs., 21, 43 (1992),

Applications Mono N-Desmethyl Disperse Polyester Dark Blue is a disperse dye for synthetic polyester fibers. It has good heat and light resistance and is used for thermal transfer recording.
References Peters A. T., et al.: J. Soc. Dyers Colour, 108(7-8), 344-8 (1992)

Applications Perindoprilat-d4 is the isotope labelled analog of Perindoprilat (P287531); an angiotensin-converting enzyme (ACE) inhibitor and antihypertensive.
References Pascard, C., et al.: J. Med. Chem., 34, 663 (1991)

Stability Hygroscopic, Light Sensitive, Temperature Sensitive
Applications Fluvastatin 3-Hydroxy-4,6-diene Sodium Salt is a metabolite of Fluvastatin (F601250), a synthetic HMG-CoA reductase inhibitor. Antilipemic.
References Yuan, J., et al.: Atherosclerosis, 87, 147 (1991), Tse, F.L.S., et al.: J. Clin. Pharmacol., 32, 630 (1992), Dain, J.G., et al.: Drug Metab. Disposit., 21, 567 (1993),

Stability Hygroscopic
Applications Sodium Stibogluconate is an intermediate used to prepare Dihydropyrido[2,3-d]pyrimidines as a new class of antileishmanial agents.
References Agarwal, A., et al.: Bioorg. Med. Chem., 13, 6678 (20050

Stability Hygroscopic
Applications 4-Chlorophenylcyanamide is an intermediate used in synthesis of N-(4-Chlorophenyl)-O-methylisourea Sulfate Salt (~90%) (C378465), which is a cytotoxic agent which displays tumor inhibitory activity.
References Hendry, J. et al.: Brit. J. Pharmacol. Chemother., 6, 201 (1951);

Applications Deschloro-2-phenylsulfonyl-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.
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)

Applications 3-Methyl Adenine-d3 is labelled 3-Methyl Adenine (M275904). 3-Methyl Adenine is a selective autophagy and phosphoinositide 3-kinase (PI3K) inhibitor (1,2,3). 3-MA inhibits autophagy by blocking autophagosome formation via the inhibition of type III Phosphatidylinositol 3-kinases (PI-3K).
References (1) Munafo, D., et al.: J. Cell Sci., 114, 3619 (2001) (2) Aggarwal, B., et al.: Biochem. Pharmacol., 71, 1397 (2006) (3) Hayat, M., et al.: Oncologist, 12, 20 (2007)