Toxicologie

Applications Eslicarbazepine acetate, (BIA 2-093), is a promising antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine. Neuroprotective & Neuroresearch product.
References Benes, J., et al.: J. Med. Chem., 42, 2582 (1999), Tong, X., et al.: Br. J. Pharmacol., 133, 867 (2001), Almeida, L., et al.: J. Clin. Pharmacol., 45, 1062 (2005), Elger, C., et al.: Epilepsia, 48, 497 (2007),

Applications Phenthoate is an organothiophosphate insecticide used against lepidoptera and houseflies.
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 Strempel, S., et al.: Envrion. Toxicol. Chem., 32, 1187 (2013); Zhao, Q. et al.: Anal. Bioanal. Chem., 405, 4765 (2013);

Applications Methionine sulfoximine inhibits both glutamine synthetase and g-glutamylcysteine synthetase. Working concentrations for inhibition of g-glutamylcysteine synthetase are 0.2-2.0 mM (52% inhibition occured at 100 mM).Methionine sulfoximine is also a toxic byproduct of nitrogen trichloride, a compound that was used to bleach unprocessed wheat flour prior to 1968. The compound has been investigated as a potential neurotoxin linked to diseases such as amyotrophic lateral sclerosis (ALS) and Parkinson’s disease.
References Griffith, O.W., and Meister, A.: J. Biol. Chem. 254, 7558 (1979), Willard-Mack, C.L., et al: Neuroscience, 71, 2, 589 (1996)

Applications 3-Piperidinopropiophenone is a mono Mannich base derived from acetophenone with antibacterial, antifungal and antitumor activity. 3-Piperidinopropiophenone shows cytotoxicity againts Jurkat cells.
References Gul, H.I. et al.: Biol. Pharmac. Bull., 26, 631 (2003); Gul, M. et al.: Arzneim.-Forsch., 51, 679 (2001); Gul, H. et al.: Arzneim.-Forsch., 51, 72 (2001);

Applications A metabolite of Aflatoxin B1; a hepatocarcinogen in many animal models and probably a human carcinogen. It is produced by the predominant forms of cytochrome P 450 enzymes responsible for the biotransformation of AFB1. It shows potential predictive value as a marker for exposure and risk of dietary aflatoxins.Environmental contaminants; Food contaminants
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 Mykkaenen, H., et al.: Int. J. Cancer, 115, 879 (2005); Van Vleet, T.R. et al.: J. Toxicol. Environ. Health, 65, 853 (2002);

Impurity Estriol EP Impurity H
Applications 16α-Hydroxy Estrone (Estriol EP Impurity H) is a major metabolite of Estradiol.
References Fishman, H.G, et al.: Biochemistry, 8, 4304 (1969), Ryan, Sugar, J., et al.: J. Clin. Endocrinol. Metab., 50, 137 (1980), Numazawa, M., et al.: Steroids, 38, 149 (1981), Travis, R., et al.: Breast Cancer Res., 5, 239 (2003),

Impurity Nicardipine USP Related Compound B
Applications A pyridine metabolite M-5 of Nicardipine. Nicardipine USP Related Compound B.
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 Triggle, A., et al.: J. Med. Chem., 23, 1442 (1980), Freedman, D., et al.: Drugs, 34, 578 (1987), Guengerich, F., et al.: Xenobiotica, 25, 689 (1995), Schleifer, K., et al.: Pharmazie, 54, 804 (1999),

Applications An oleic acid synthetic analog that is an effective non-toxic anticancer drug with a wide spectrum against different types of cancer. An antihypertensive.
References Llado, V. et al.: J. Cell. Molec. Med., 14, 659 (2010); Alemany, R. et al.: J. Lip. Res., 47, 1762 (2006); Martinez, J. et al.: J. Pharmacol. Exp. Therap., 315, 466 (2005);

Impurity Betamethasone Dipropionate EP Impurity G
Applications Betamethasone Tripropionate (Betamethasone Dipropionate EP Impurity G) is a Betamethasone (B327000) related compound.
References Grootveld, M., et al.: Biochem. Pharmacol., 37, 271 (1988), Chen, B., et al.: Steriods, 74, 30 (2009), Mikami, E., et al.: J. Pharm. Biomed. Anal., 28, 261 (2002),

Applications Potassium bromide is an ionic compound that is commonly used in chemistry to form a pellet that can be used to analyze a number of compounds by means of infrared spectroscopy. Potassium bromide is also used as an anticonvulsant to treat refractory seizures in humans and dogs.
References Kirkland, J.: Anal. Chem., 27, 1537 (1955); Korinthenberg, R., et al.: J. Child Neuro., 22, 414 (2007); Wilberley, S., et al.: Anal. Chem., 29, 210 (1957); Yohn, S., et al.: J. Am. Vet. Med. Ass., 201, 468 (1992)

Applications Atorvastatin (A791750) impurity.
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996);

Applications 17β-neriifolin could be considered a candidate for the treatment of hepatocellular carcinoma. It can also work as an inhibitor of hERG channel trafficking.
References Zhao, Q., et al.:Fitoterapia, 82, 735 (2011); Wang, L., et al.: J. Pharmacol. Exper. Ther., 320, 525 (2007)

Stability Temperature and Light Sensitive, unstable in solution
Applications Vitamin K1 Hydroxide is a derivative of Vitamin K1 (V676080), which occurs widely in green plants, algae, and photosynthetic bacteria.
References Hassan, M.M.A., et al.: Anal. Profiles Drug Subs., 17, 449 (1988), Breton, J., et al.: Biochemistry, 33, 12405 (1994), Dowd, P., et al.: Science, 269, 1684 (1995),

Stability Hygroscopic
Applications Antihistaminic.
References Berthon, B., et al.: Biochem. Pharmacol., 47, 789 (1994), Hu, Q., et al.: J. Biol. Chem., 274, 33995 (1999),

Applications A labelled nonsteroidal anti-inflammatory drug (NSAID); activity resides primarily in the (S)-isomer.
References Busson, M., et al.: J. Int. Med Res., 14, 53 (1986), Meade, E.A., et al.: J. Biol. Chem., 268, 6610 (1993), Davies, N.M., et al.: Clin. Pharmacokinet., 34, 101 (1998),

Applications Inhibits the enzyme HMG-CoA reductase in vitro.
References Endo, A., et al.: J. Antibiot., 32, 852 (1979), Alberts, A.W., et al.: Drug Invest., 2 (Suppl. 2), 9 (1990), Kuroda, M., et al.: Biochim. Biophys. Acta, 486, 70 (1977),

Applications A Rosuvastatin (R700500) intermediate as HMG-CoA reductase inhibitor.
References Beck, et al.: J. Med. Chem., 33, 52 (1999),

Applications An Epinephrine (E588585) derivative formed in injection solutions and eye drops during sterilization and storage of L-Epinephrine Bitartrate.
References De Mol, N.J. et al.: Pharmac. Week., 117, 1 (1982); Liu, C. et al.: Yao. Fen. Zaz., 2, 200 (1982);

Stability Hygroscopic, Temperature Sensitive
Applications Gemcitabine Triphosphate is a phosphorylated metabolite of Gemcitabine (G305000), an antineoplastic agent.
References Kennedy., E.P., et al.: J. Biol. Chem., 222, 193 (1956),

Impurity Rosuvastatin EP Impurity C (Calcium Salt)
Stability Hygroscopic
Applications 5-Oxo Rosuvastatin (Rosuvastatin EP Impurity C (Calcium Salt)) is a Rosuvastatin (R700500) impurity.
References Endo, A., et al.: J. Antibiot., 32, 852 (1979), Beck, G., et al.: J. Med. Chem., 33, 52 (1990), Koga, T., et al.: Lipids, 30, 775 (1995),

Applications di(2-Hydroxy Atorvastatin) Calcium Salt is a metabolite of Atorvastatin Calcium Salt (A791750), a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996); Whitfield, L.R., et al.: Eur. J. Drug Metab. Pharmacokinet., 25, 97 (2000)

Applications A novel semi-synthetic taxane with antitumor activity used for the treatment of castration-resistant prostate cancer. A microtubule inhibitor.
References Agarwal, N. et al.: Fut. Oncol., 7, 15 (2011); Mita, A. et al.: Clin. Cancer Res., 15, 723 (2009); Figg, W.D. et al.: Cancer Biol. Ther., 10, 1233 (2010);

Applications Nicergoline-d3 is the labeled analogue of Nicergoline(N394550), a drug used for age-dependent cognitive impairment such as Alzheimers disease and other types of dementia.
References Caraci, F., et. al.: Brain Res., 1047, 30 (2005); Mizuno, T., et. al.: Brain Res., 1066, 78 (2005)

Applications A metabolite of Clomipramine.
References McTavish, D., et al.: Drugs, 39, 136 (1990), Chauret, N., et al.: Drug Metab. Dispos., 25, 1130 (1997), Gex-Fabry, M., et al.: Ther. Drug Monit., 22, 701 (2000), Herrera, D., et al.: J. Clin. Pharmacol., 40, 1488 (2000),

Impurity Bisoprolol EP Impurity L (Metoprolol EP Impurity C)
Stability Hygrscopic
Applications 4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]benzaldehyde (Bisoprolol EP Impurity L (Metoprolol EP Impurity C)) is a Metoprolol impurity .
References Baldwin, J.J. , et al.: J. Med. Chem., 29, 1065 (1986), Ravelet, C., et al.: J. Sep. Sci., 29, 1322 (2006),

Applications A metabolite of Triamcinolone acetonide.
References Edsbacker, S., et al.: Drug Metab. Dispos., 11, 590 (1983), Szefler, S., et al.: Eur. J. Clin. Pharmacol., 30, 323 (1986), Hansel, T., et al.: J. Immunol. Methods, 145, 105 (1991), Argenti, D., et al.: J. Clin. Pharmacol., 39, 695 (1999),

Impurity Amlodipine EP Impurity F / Amlodipine USP Related Compound F
Applications Amlodipine Besilate (A633500) impurity. Amlodipine EP Impurity F
References Coburn, R., et al.: J. Med. Chem., 31, 2103 (1988), Gupta, S., et al.: Eur. J. Med. Chem., 38, 867 (2003), Vazzana, I., et al.: J. Med. Chem., 50, 334 (2007),

Impurity Calcium Folinate Hydrate EP Impurity E
Stability Unstable in Basic Solution
Applications 5-Formyltetrahydropteroic Acid is an impurity of Folic Acid (F680300); a vitamin needed to synthesize DNA, conduct DNA repair and methylate DNA. It also acts as a cofactor in biological reactions involving folate.
References Xu, L., et al.: Mol. Pharm., 7, 1311 (2010); Everette, J., et al.: J. Agric. Food Chem., 58, 8139 (2010); Alshatwi, A., et al.: Food, Chem., Toxicol., 48, 1881 (2010); McKay, D., et al.: Nut. J., 9 (2010)

Impurity Propofol EP Impurity E; Propofol USP Related Compound A
Applications Dipropofol (Propofol EP Impurity E) is a dimeric derivative of Propofol (P829750). Dipropofol is an antibacterial agent with strong activity againts Gram-positive bacteria. Dipropofol also displays antioxidant and radical scavenging activity. Propofol USP Related Compound A.
References Ogata, M. et al.: Chem. Pharm. Bull., 53, 344 (2005); Ogata, M. et al.: Biol. Pharmac. Bull., 30, 1565 (2007);

Applications Diltiazem (D460620) intermediate (impurity B).
References Chaffman, M., et al.: Drugs, 29, 387 (1985), Kamath, B., et al.: J. Pharm. Biomed. Anal., 11, 407 (1993), Chankvetadze, B., et al.: J. Pharm. Biomed. Anal., 27, 161 (2002),

Impurity Fluticasone USP Related Compound B
Applications An impurity of Fluticasone Propionate (F599500), a derivative of Flumethasone (F455000). An antiallergic; anti-asthmatic; anti-inflammatory. Fluticasone USP Related Compound B.
References Matuszewski, B, et al.: Anal. Chem., 75, 3019 (2003), Fekete, S., et al.: J. Pharm. Biomed. Anal., 49, 64 (2009), Meltzer, E.O., et al.: J. Allergy Clin. Immunol., 86, 221 (1990), Mitchison, H.C., et al.: Gut, 32, 260 (1991), Phillipps, G.H., et al.: J. Med. Chem., 37, 3717 (1994)

Impurity Tranexamic EP Impurity A
Applications Tranexamic Acid Dimer (Tranexamic EP Impurity A) is a Tranexamic Acid (T714505) impurity.

Stability Hygroscopic
Applications A metabolite of Cortisol (H714615).
References Quinkler, M., et al.: J. Clin. Endocrinol. Metab., 88, 2384 (2003), Draper, N., et al.: J. Endocrinol., 186, 251 (2005), Kotlowska, A., et al.: Clin. Biochem., 42, 448 (2009),

Impurity Fluocinolone Acetonide EP Impurity E
Stability Hygroscopic
Applications (6α,9β,11β,16α)-9,11-Epoxy-6-fluoro-21-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]pregna-1,4-diene-3,20-dione, can be used in the production of fluocinolone acetonide (F455800).
References Grinenko, G.S, Khimiko-Farmatsevticheskii Zhurnal, 12, 110 (1978), Sammul, et al.: J. Assoc. Off. Agric. Chem., 47, 952 (1964), Emerson, M.V., et al.: BioDrugs, 21, 245 (2007),

Applications Telocinobufagin is isolated as a major component from skin secretion of the toad Bufo rubescens. Telocinobufogenin is a novel antibiotic cardiotonic.
References Akizawa, T., et al.: Chem. Pharm. Bull., 42, 754 (1994); Hancock, R., et al.: Antimicrob. Agents Chemother., 43, 1317 (1999); Jing, Y., et al.: J. Cancer Res., 85, 645 (1994); Kamano, Y., et al.: J. Med. Chem., 45, 5440 (2002); Schoner, W., et al.: Eur. J. Biochem., 269, 2440 (2002); Cunha Filho, G., et al.: Toxicon, 45, 777 (2005)

Applications The 5-hydroxy analogue of the bronchodilator, Albuterol (A514500).

Applications (-)-Biotin Sulfoxide, is a metabolite of Biotin (B389040), which is a growth factor present in minute amounts in every living cell, and plays an indispensable role in numerous naturally occurring carboxylation reactions.
References du Vigneaud, et al.: J. Biol. Chem., 146, 475 (1942), Traub, et al.: Nature, 178, 649 (1956), Siegel, H., et al.: Experienta, 37, 789 (1981), Vesely, D.L., Science, 216, 1329 (1982), Hugues, M., et al.: Biochemistry, 31, 12 (1992),

Applications A metabolite of Mifepristone (M343975).
References Ringler, I., et al.: Metabolism, 13, 37 (1964), Gagne, D., et al.: J. Steroid. Biochem., 25, 315 (1986), Jang, G., et al.: Biochem. Pharmacol., 52, 753 (1996), Hild, S., et al.: Hum. Reprod., 15, 822 (2000), Gainer, E., et al.: Steroids, 68, 1005 (2003),

Applications A labelled inhibitor of glucose synthesis.
References Garcia-Salguero, L. et al.: Arch. Int. Physiol., Biochim. Biophys., 99, 237, (1991); Martirosyan, A., et al.: Biochem. Pharmacol., 68, 1729 (2004);

Stability Hygroscopic
Applications 3-Sulfoglycolithocholic Acid Disodium Salt is a derivative of Lithocholic acid (L469180). Lithocholic acid (LCA) is a putative tumor promoter,that is shown to be able to inhibit mammalian DNA polymerase β.
References Ogawa, A., et al.: Jap. J. Canc. Res., 89, 1154 (1998)

Impurity Carvedilol EP Impurity B; Carvedilol Impurity B; Carvedilol USP B
Applications Carvedilol Bis-carbazole (Carvedilol EP Impurity B; Carvedilol Impurity B; Carvedilol USP B) is an impurity from the process of Carvedilol (C184625).

Applications A metabolite of Desogestrel.
References Back, D., et al.: Br. J. Clin. Pharmacol., 26, 23 (1988), Wienkers, L., et al.: Drug Metab. Dispos., 1990, 24, 610 (1990), Bourrie, M., et al.: J. Pharmacol. Exp. Ther., 277, 321 (1996), Ono, S., et al.: Xenobiotica, 26, 681 (1996),