Toxicologie

Applications Cholesterol-d6 has been used in safe procedures to measure the percentage of cholesterol absorption, based on that of D. B. Zilversmit (1972), by using Cholesterol-d6 as a stable nonradioactive isotopic tracer of cholesterol that was administered orally into normal individuals to facilitate clinical investigation.
References Bosner, Matthew S., Journal of Lipid Research, 34, 1047-53, (1993)

Applications L-Propoxyphene-d5 Hydrochloride is the isotope labelled analog and L-isomer of Propoxyphene Hydrochloride (P831500); a controlled substance (opiate) and analgesic (narcotic). The α-DL-and D-diastereoisomers possess marked analgesic activity in contrast to the β-diastereoisomers which are substantially inactive. Oral administration of L-Propoxyphene Hydrochloride enhances the analgesic activity of D-Propoxyphene Hydrochloride.
References Goldenthal, E.I., et al.: Toxicol. Appl. Pharmacol., 18, 185 (1971); McEwan, B., et al.: Anal. Profiles Drug Subs., 1, 301 (1972); Murphy, P.J., et al.: J. Pharmacol. Exp. Ther., 199, 415 (1976)

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

Applications A prototypical BCRP inhibitor. Inhibits the Bcrp1-mediated transport.
References Neville, K., et al.: Clin. Cancer Res., 10, 2525 (2004), Reardon, D., et al.: J. Clin. Oncol. 23, 9359 (2005), Pan, G., et al.: Drug Metab. Dispos., 35, 1165 (2007),

Applications Protected Fluvoxamine.

Applications 3-Fluoro-2-methoxy-benzenesulfonyl-d3 Chloride is the isotope labelled analog of 3-Fluoro-2-methoxy-benzenesulfonyl Chloride (F593265), which is a derivative of 2-Fluoroanisole (F587670); a useful synthetic intermediate with antifungal activity.
References Pinto, M. F. S., et al.: J. Mol. Struc.: Theochem., 539, 303-310 (2001)

Applications Azadiradione is an extract from Neem (Azadirachta indica) plant and may contain antifungal properties. It has also been shown to restore protein quality control and ameliorate disease pathogenesis in Huntington’s disease.
References Singh, T. et al.: Am. J. PharmTech. Res., 6, 323 (2016); Singh, B. et al.: Mol. Neurobiol., 55, 6337 (2018);

Applications 8-Hydroxybentazone, is a metabolite of Bentazon, a selective post-emergence herbicide.
References Kim, J., et al.: ACS Symp. Series, 899, 92 (2005); Roper, J., et al.: Wat. Res., 29, 2720 (1995);

Applications Labelled analogue of Dibenz[a,h]anthracene, a polycyclic aromatic hydrocarbon (PAH) and a known carcinogen. Dibenz[a,h]anthracene has produced positive results in bacterial DNA damage and mutagenicity assays and in mammalian cell DNA damage, mutagenicity and cell transformation assays.
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 Farmer, P.B. et al.: Mutat. Res. Re. Mutat. Res., 544, 397 (2003); Leadon, S. et al.: Carcinogenesis, 16, 3021 (1995); Andrews, A.W. et al.: Mutat. Res., 51, 311 (1978); Kaden, D.A. et al.: Cancer Res., 39, 4152 (1979);

Stability Hygroscopic
Applications Desfuroyl Ceftiofur Dimer is an impurity of the drug Ceftiofur (C244695), a third generation cephalosporin antibiotic used in veterinary medicine.
References Donaldson, S.C. et al.: Appl. Environ. Microbiol., 72, 3940 (2006); Yancey, R.J. et al.: Am. J. Vet. Res., 48, 1050 (1987);

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.

Applications 3-Bromopropionic-2,2,3,3-d4 Acid is the labeled analog of 3-Bromopropionic acid (B687705). 3-Bromopropionic Acid is used as a reagent in the synthesis of nitrogen containing diselenides which exhibit antioxidant activity. Also used as a reagent in the synthesis of indolin-2-one-based multi-targeted receptor tyrosine kinase inhibitors as potential anticancer agents.
References Nascimento, V., et al.: Eur. J. Med. Chem., 87, 131 (2014); Zhang, L., et al.: Eur. J. Med. Chem., 82, 139 (2014)

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 Labelled Azathioprine (A803350). An immunosuppressive antimetabolite. Also active as disease modifying antirheumatic drug (DMARD).
References Mitrou, P.S., et al.: Arzneim.-Forsch., 29, 483, 662 (1979), Ding, T.L., et al.: Drug. Metab. Dispos., 7, 373 (1979), Chan, G.L.C., et al.: Pharmacotherapy, 7, 165 (1987), Sandborn, W.J., et al.: : Scand. J. Gastroenterol., 33, Suppl. 225, 92 (1998,)

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.

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 Labelled (6R,7S)-Cefoperazone (C242890). (6R,7S)-Cefoperazone is the enantiomer of Cefoperazone (C242900) as an impurity.
References Fabre, H., et al.: J. Pharm. Sci., 73, 611 (1984), Strasters, J., et al.: Anal. Chem., 63, 2503 (1991), Chen, Z., et al.: World Notes Antibiot., 25, 249 (2004),

Applications (S)-7-Hydroxy Efavirenz, is a metabolite of Efavirenz (E425000), a nonnucleoside HIV-1 reverse transcriptase inhibitor. Antiviral.
References Young, S.D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995),

Applications Difluoro Atorvastatin Acetonide tert-Butyl Ester is a useful synthetic intermediate in the synthesis of Difluoro Atorvastatin (D445660); an Atorvastatin impurity.
References Dart, A., et al.: Am. J. Cardiol., 80, 39 (1997)

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 2,4'-Dibromobenzophenone (CAS# 78281-59-1) is a useful research chemical compound.

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 L-Xylose is part of the chemical profile of a polysaccharide extracted in aquatic life that shows anti-viral activites against herpes simplex virus 1 & 2 as well as influenza A virus. This is the L-[13C5]Xylose labeled analog.
References Lee, J.B. et al.: Biol. Pharm. Bullet., 29, 2135 (2006);

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 Deacetylvinblastine hydrazide sulfate salt is the sulfate salt of Deacetylvinblastine hydrazide, a cytotoxic vinca alkaloid often conjugated with folic acid to produce EC145, a novel folate-receptor targeted agent that is currently under development as an anti-cancer agent.
References Pribble, P. & Edelman, M.: Expert Opin. Invest. Drugs, 21, 755 (2012); Reddy, J., et al.: Cancer Res., 67, 4434 (2007); Roy, M., et al.: Dev. Biol Stand., 74, 323 (1991)

Applications Protected rac Zearalenone-d6

Applications 7,8,9,10-Tetrahydro-8-methyl-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine is a secondary amine drug varenicline impurity. It is a part of the pharmaceutical formulation of varenicline tartrate tablet.
References Waterman, K., et al.: J. Pharm. Sci., 97, 1499 (2008); Watheesh, B., et al.: Acta Chromatogr., 22, 207 (2010);

Applications CP 55,940 is a cannabinoid agonist which is considerably more potent than Δ9-THC in both behavioral tests and receptor binding assays. Displays high and roughly equal affinity for both central and peripheral cannabinoid receptors (Ki = 0.6 - 5.0 and 0.7 - 2.6 nM at CB1 and CB2 respectively; EC50 values are 0.2, 0.3 and 5 nM at CB1, CB2 and GRP55 respectively).Controlled substance. Synthetic Cannabinoids
References Wiley, et al.: Neuropharmacology, 34, 669 (1995); Griffin, et al.: J. Pharmacol. Exp. Ther., 285, 553 (1998); Thomas, et al.: J. Pharmacol. Exp. Ther., 285, 285 (1998); Ryberg, et al.: Br. J. Pharmacol., 152, 1092 (2007);

Applications Mometasone Furoate-d8 is the isotope labelled analog of Mometasone Furoate (M490000); a topical corticosteroid used as an anti-inflammatory.
References Shapiro, E.L., et al.: J. Med. Chem., 30, 1581 (1987); Graft, D., et al.: J. Allergy Clin. Immunol., 98, 724 (1996)

Applications (4S)-4-Hydroxy Pravastatin Lactone is an intermediate in the synthesis of Pravastatin 6'-Ketone Sodium Salt (P702050), which is an impurity of Pravastatin Sodium (P702000), which is a competitive inhibitor of HMG-CoA reductase. It can be used as a drug to for lowering cholesterol and preventing cardiovascular disease.
References Serizawa, N., et al.: J. Antibiot., 36, 604 (1983), Yoshino, G., et al.: Lancet, 2, 740 (1986), White, H.D, et al.: N. Engl. J. Med., 343, 317 (2000);

Applications Dinocap is an acaricide and pesticide.
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 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 3,5-Dibromo-4-hydroxybenzonitrile-2,6-d2 (CAS# 1219798-95-4) is a useful isotopically labeled research compound.

Applications Controlled substance. CNS stimulant. The less potent threo-enantiomer of Methylphenidate. The threo enantomers have shown that the pharmacological activity residues predominantly in the d-threo enantiomer.
References Greenblatt, E.N., et al.: J. Pharmacol. Exp. Ther., 131, 115 (1961), Padmanabhan, G.R., et al.: Anal. Profiles Drug Subs., 10, 473 (1981), Kuczenski, R., et al.: J. Pharmacol. Exp. Ther., 296, 876 (2001), Pelham, W.E., et al.: J. Consult. Clin. Psychol., 61, 506 (1993), Srinivas, N.R., et al.: Pharm. Res., 10, 14 (1993),

Applications Tridihexethyl Chloride, is an anticholinergic, antimuscarinic and antispasmodic drug.
References Gohil, V., et al.: Nature Biotech., 28, 249 (2010); Rider, J. A., et al.: Curr. therap. Res., 20, 142 (1976);

Applications Clemizole Hydrochloride inhibits Hepatitis C RNA replication in cell culture through the suppression of the binding between the nonstructural protein 4B and the viral RNA genome with little toxicity for the host cell. Clemizole Hydrochloride is also a potent inhibitor of transient receptor potential channel TRPC5.
References Einav, S., et al.: Nat. Biotechnol., 26, 1019 (2008); Richter, J. M., et al.: Mol. Pharmacol., 86, 514 (2014)

Applications Labelled Testosterone ester.
References Ruelle, P., et al.: Int. J. Pharm., 157, 219 (1997), de la Torre, X., et al.: J. Pharm. Biomed. Anal., 24, 645 (2001), Adat, S., et al.: Lett. Drug Des. Discov., 1, 334 (2004),

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 Efavirenz 1-Desamine-1-oxy is an analog of Efavirenz (E425000), a nonnucleoside HIV-1 reverse transcriptase inhibitor. Antiviral.
References Young, S.D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995)

Applications Estradiol 17β-sulfate is a naturally occuring steroid in whihc can be converted into Estradiol(E888000)
References Takanashi, K., et al.: Steroids., 68, 383-392 (2003)

Applications L-Carnitine-15N is an isotopically labelled analog of L-Carnitine (C184110), which is an essential cofactor of fatty acid metabolism; required for the transport of fatty acids through the inner mitochondrial membrane. Synthetized primarily in the liver and kidney; highest concentrations found in heart and skeletal muscle.
References Mitchell, M.E., et al.: Am. J. Clin. Nutr., 31, 293 (1978); Lango, R., et al.: Cardiovasc. Res., 51, 21 (2001);Vaz, F.M., et al.: Biochem. J., et al.: 361, 417 (2002);Karlic, H., et al.: Nutr. J., 20, 709 (2004)