Toxicologie

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);

Applications Cyclizine is a piperazine derivative with anti-emetic activity that is useful in the prevention and treatment of nausea and vomiting associated with motion sickness. Antiemetic.
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 Kuntzman, R., et al.: J. Pharmacol. Exp. Ther., 158, 332 (1967), Walker, R., et al.: Eur. J. Pharm. Sci., 4, 301 (1996), Dumasia, M., et al.: Xenobiotica, 32, 795 (2002),

Impurity Valproic Acid USP Related Compound A
Applications Diallylacetic Acid (Valproic Acid USP Related Compound A), is a metabolite of Valproic Acid (V094750) as anticonvulsant agents. It can also be used for the synthesis of Velbanamine.
References Liu, H., et al.: Beilstein J. Org. Chem., 9, 983 (2013); Loscher, W., Prog. Neurobiol., 58, 31 (1999); Netzeva, T., et al.: Pharmac. Res., 17, 727 (2000);

Applications Isometheptene Maleate belongs to a group of sympathomimetic amine and shows very little antihypertensive activity. Isometheptene Maleate is used as an antispasmodic drug.
References Vidrio, H. et al.: J. Pharmacol. Exp. Therap., 187, 308 (1973); Taylor, W.G. et al.: Drug Metab. Disp., 5, 564 (1977);

Applications A synthetic adrenocorticosteroid that acts as an anti-inflammatory and anti-pruritic agents. It is used as a topical for the treatment of dermatologic disorders such as atopic dermatitis and psoriasis.
References Mason, J. et al.: Br. J. Dermatol., 146, 351 (2002); Sears, H.W. et al.: Clin. Therap., 19, 710 (1997); Otomo, Y.Z. et al.: Nip. Yakur. Zas., 78, 647 (1981);

Applications 2-[3-(Aminosulfonyl)-4-chlorobenzoyl]-benzonic Acid is a potential metabolite of Chlorthalidone.
References Salado C., et al.: J. Chromatography. Biomed. App., 690, 195 (1997);

Applications 2-Oxo-Zoniporide is an metabolite of Zoniporide, a potent and selective inhibitor of human sodium-hydrogen exchanger isoform1(NHE-1) and protects against cardiac ischemia-reperfusion injury.
References Ross, T.W., et al.: Cardiovascular. Drug. Reviews., 21, 17 (2003); Deepak, D., et al.: Drug. Metabol. Dispos., 38, 641 (2010);

Applications 3-Cysteinylacetaminophen-D5 (major), Trifluoroacetic Acid Salt is deuterium labeled 3-Cysteinylacetaminophen Trifluoroacetic Acid Salt (C994750), which is a metabolite of Acetaminophen (A161220), an analgesic and antipyretic agent used as a pain reliever to treat headache, muscle aches, and arthritis (1,2,3).Minimum isotopic incorporation d-3, no d-0 present. A representative lot has 64% isotopic incorporation at the 6-position, 89% at the 4-position.
References (1) McGill, M. R. and Jaeschke, H. Pharm Res. 30, 2174 (2013)(2) Fairbrother, J.E., et al.: Anal. Profiles Drug Subs., 3, 1 (1974) (3) Hinson, J.A., et al.: Rev. Biochem. Toxicol., 2, 103 (1980)

Applications Campesteryl Ferulate is a component of γ-​oryzanol with antioxidant activities.
References Xu, Z., et al.: J. Agric. Food Chem., 49, 2077 (2001);

Applications Methyl Lithocholate is an derivative of Lithocholic Acid (L469180),a cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones.
References Roleira, F.M., et al.: Lett. Drug. Design. Discovery., 7, 610 (2010);

Applications Labelled Ouabain (O714500). A cardiac glycoside that inhibits Na(+)/K(+) ATPase. It regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1.
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 Padilha, A.S. et al.: Clin. Exp. Pharmacol. Physiol., 35, 801 (2008); Blaustein, M.P. et al.: Clin. Exp. Hypertens. 20, 691 (1998); van Huysse, J.W. et al.: Clin. Exp. Hypertens. 20, 657 (1998);

Impurity Ethinylestradiol EP Impurity H
Applications A degradation product of Ethynyl Estradiol (EE), (E685100).
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

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),

Applications 5α-Pregnane-3β,20(S)-diol, is a metabolite of Progesterone (P755900).
References Beall, et al.: Biochem. J., 31, 35 (1937), Okuda, A., et al.: J. Biol. Chem., 259, 7519 (1984), Russell, D., et al.: Biochemistry, 31, 4737 (1992), Kondo, K., et al.: Eur. J. Biochem., 219, 357 (1994), Westerbacka, J., et al.: J. Clin. Endocrinol. Metab., 88, 4924 (2003),

(1α)-17-(Acetyloxy)-6-chloro-1-(chloromethyl)-pregna-4,6-
diene-3,20-dione; 6-Chloro-1α-(chloromethyl)-17-
hydroxypregna-4,6-diene-3,20-dione Acetate; Cyproterone
Acetate EP Impurity C

Applications Carvedilol (C184625) derivative.
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 A metabolite of Acepromazine (A130900).
References Cossum, P., et al.: Drug Dispos., 9, 321 (1988), Stowell, L., et al.: J. Anal. Toxicol., 22, 166 (1998),

Applications Diazoxide-d3 is the labeled analogue of Diazoxide (D417305), which reduces status epilepticus neuron damage in diabetes.
References Baba, A., et al.: J. Neurosci., 23, 7737 (2003); Bancila, V., et al.: J. Neurochem., 90, 1243 (2004); Bancila, V., et al.: J. Biol. Chem., 280, 8793 (2005)

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)

Stability Hygroscopic
Applications (Z)-11-(3-(Dimethylamino)propylidene)-6,11-dihydrodibenzo[b,e]oxepine-2-carbaldehyde Hydrochloride, is a metabolite of Olopatadine (O575000), a dual acting histamine H1-receptor antagonist and mast cell stabilizer. Antiallergic; antihistaminic.
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 Kamei, C., et al.: Arzneim.-Forsch., 45, 1005 (1995), Sharif, N.A., et al.: J. Pharmacol. Exp. Ther., 278, 1252 (1996), Abelson, M.B., et al.: Am. J. Ophthalmol., 125, 797 (1998),

Applications Used as an antihypertensive and antianginal.
References Gross, G.J., et al.: Gen. Pharmacol., 14, 677 (1983), Molyvdas, P.A. and Sperelakis, N.: J. Cardiovasc. Pharmacol., 8, 449 (1986), Mizuno, K., et al.: Res. Comm. Chem. Pathol. Pharmacol., 52, 3 (1986)

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 dextrorotatory stereoizomer of Quinine. Antiarrhythmic (class IA). Antimalarial.
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 Loutfy, M.A., et al.: Anal. Profiles Drug Subs., 12, 483 (1983), Mason, J. W., et al.: Ann. N. Y. Acad. Sci., 432, 162 (1984),

Stability Light Sensitive
Applications β-Cembrenediol is an inhibitor of tumor promotion. Novel c-Met inhibitors which are used in anticancer treatments.
References Le-Huu, P. et al.: ChemCatChem., 8, 3755 (2016); Ebrahim, H. et al.: Bioorg. Med. Chem., 24, 5748 (2016);

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 Methyltriphenylphosphonium Bromide is a lipophilic molecule with a cation allowing for it to be used to deliver molecules to specific cell components. Also considered an antineoplastic agent.
References Selassie, C.D. et al.: J. Med. Chem., 33, 1914 (1990); Venkatachalam, M.A et al.: Kidney Int., 49, 449 (1996);

Stability Hygroscopic
Applications A metabolite of Equilin (E592800).
References Enmark, E., et al.: J. Clin. Endocrinol. Metab., 82, 4258 (1997), Wang, Z., et al.: J. Med. Chem., 43, 2419 (2000), Jiang, X., et al.: Steroids, 71, 334 (2006),

Applications A metabolite of Cholesterol.
References Connor, W., et al.: J, Clin. Invest., 48, 1363 (1969), Nestel, P., et al.: Metabolism, 24, 189 (1975), Ellegard, L., et al.: Eur. J. Clin. Nutr., 45, 451 (1991), Pedersen, A., et al.: J. Lipid Res., 41, 1901 (2000),

Applications A metabolite of Cortisone (C696500).
References Mashkovskii, M., et al.: Med. Agents, 2, 34 (2002),

Applications 4-Hydroxyatorvastatin is a hydroxylated metabolite of Atorvastatin, 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 Smith, S. et al.: Am. J. Cardiol., 80, 10H (1997); Jacobsen, W. et al.: Drug Metab. Dispos., 28, 1369 (2000); Istvan, E. et al.: Science, 292, 1160 (2001); Tabernero, L. et al.: J. Biol. Chem., 278, 19933 (2003); Bratton, L. et al.: Bioorg. Med. Chem., 15, 5576 (2007);

Impurity Betamethasone Dipropionate EP Impurity D
Applications Betamethasone 21-acetate-17-propionate (Betamethasone Dipropionate EP Impurity D) is a related compound of Betamethasone dipropionate (B327005).
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 A metabolite of Spironolactone.
References Gochman, N., et al.: J. Pharmacol. Exp. Ther., 135, 312 (1962), Tori, K., et al.: Steroids, 4, 713 (1964), Solymoss, B., et al.: Toxicol. Appli. Pharmacol., 18, 586 (1971),

Applications Physiological analog of vitamin B12 where the CN group is replaced with OH. Exists in aqueous solution as an equilibrium mixture of the hydroxy isomer and the ionic aqua isomer (aquacobalamin). Precursor of the coenzymes methylcobalamin and cobamamide. Coordination Compound. Vitamin (hematopoietic).
References Kaczka, E.A., et al.: Science, 112, 354 (1950), Friedrich, W., et al.: Vitamins, 837 (1988), Forsyth, J.C., et al.: Clin. Toxicol., 31, 277 (1993),

Applications Triterpenoid which can inhibit the proliferation of leukemia HL-60 cells.
References Cho, J., et al.: Pulmon. Pharmacol. Ther., 23, 190 (2010), Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010), Saha, S., et al.: J. Agric. Food Chem., 58, 434 (2010),

Applications 2-Azidoethanol is used as a reagent in the glycosylation of mono- or polysaccharides. 2-Azidoethanol is also used as a 2’-deoxy-ethynyluridine (EdU) blocker in nuclear DNA, preventing cross reactivity with other antibodies in order to better study its related pathways in the body.
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 Liboska, R., et al.: PLOS ONE, 7, e51679 (2012); Sun, X., et al.: Biomacromolecules, 3, 1065 (2002)

Impurity Ezetimibe Tetrahydropyran Impurity
Applications Ezetimibe (E975000) tetrahydropyran impurity.

Applications Atorvastatin Derivative

Applications A new Sildenafil (S435000) analogue.
References Balayssac, S., et al.: J. Pharm. Biomed. Anal., 50, 602 (2009),

Impurity Fluticasone EP Impurity D
Applications Ticabesone Propionate is an impurity of Fluticasone, an antiallergic, anti-asthmatic and anti-inflammatory agent.
References Marrero-Ponce, Y., et al.: Europ. J. Med. Chem., 46, 5736 (2011); Dalvi, P., et al.: J. Chem., 20, 187 (2008);

Applications Ethylphenidate Hydrochloride is the transesterification metabolite of Methylphenidate (M325880) and ethanol.
References Patrick, K.S., et al.: J. Med. Chem., 48, 2876 (2005); Naito, T., et al.: Chem. Pharma. Bull., 12, 588 (1964);

Applications Testosterone Cypionate is an anabolic steroid with androgenic properties. Testosterone Cypionate is used for testosterone therapy in males with hypogonadism.Controlled Substance.
References Rabkin, J. G., et al.: J. Clin. Psychopharmacol., 19, 19 (1999); Hajjar, R., et al.: J. Clin. Endocrinol. Metab., 82, 3793 (1997); Rhoden, E., et al.: J. Sex Med., 7, 277 (2010);