Toxicologie

<p>Applications The major metabolite of Deflazacort.<br>References Bernareggi, A., et al.: J. Pharma. Biomed. Anal., 5, 177-81 (1987), Assandri, A., et al.: Xenobiotica, 13(3), 185 (1983), Martinelli, E., et al.: Drug Metab. Dispos., 7, 335 (1979),<br></p>

<p>Applications A metabolite of Tramadol.<br>References Lintz, V.W., et al.: Arzneim.-Forsch./Drug Res., 31, II, 11, 1932 (1981)<br></p>

<p>Stability Temperature and Light Sensitive, unstable in solution<br>Applications Vitamin K1 Hydroxide is a derivative of Vitamin K1 (V676080), which occurs widely in green plants, algae, and photosynthetic bacteria.<br>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),<br></p>

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

<p>Applications A major metabolite of Irinotecan.<br>References Canal, P., et al.: J. Clin. Oncol., 14, 2688 (1996), Haaz, M., et al.: Cancer Res., 58, 468 (1998), Kehrer, D., et al.: Clin. Cancer Res., 6, 3451 (2000), Hanioka, N., et al.: Xenobiotica, 31, 687 (2001), Satoh, T., et al.: Drug Metab. Dispos., 30, 488 (2002),<br></p>

<p>Applications 6β-Hydroxy Betamethasone can be used as analyte in analytical study for detecting betamethasone metabolites in human urine using liquid chromatography coupled to tandem mass spectrometry.<br>References Matabosch, X., et al.: Drug Testing and Analysis, 7, 663-672 (2015)<br></p>

<p>Applications The major metabolite of Boldenone, an anabolic steroid.<br>References Fotsis, T., et al.: J. Steroid Biochem., 28, 203 (1987), Song, Y., et al.: Arch. Pharm. Res., 23, 599 (2000), Buiarelli, F., et al.: Anal. Chim. Acta, 526, 113 (2004), Poelmans, S., et al.: Food Addit. Contam., 22, 808 (2005),<br></p>

<p>Impurity Clonidine EP Impurity A<br>Applications 1-Acetyl-2-imidazolidinone (Clonidine EP Impurity A) is a synthetic reagent used in the preparation of triple [14C]-labelled moxonidine which is an antihypertensive compound.<br>References Czeskis, B., et al.: J. Labelled Comp. Radiopharm., 47, 699 (2004)<br></p>

<p>Applications The main phase I metabolites of Azelastine.<br>References Adusumalli, V., et al.: Drug Metab. Dispos, 20, 530 (1992), Mano, N., et al.: J. Pharm. Biomed. Anal., 12, 557 (1994), Baldwin, S., et al.: Xenobiotica, 25, 261 (1995), Kobayashi, K., et al.: J. Pharmacol. Exp. Ther., 280, 927 (1997),<br></p>

<p>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.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>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),<br></p>

<p>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.<br>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)<br></p>

<p>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.<br>References Caraci, F., et. al.: Brain Res., 1047, 30 (2005); Mizuno, T., et. al.: Brain Res., 1066, 78 (2005)<br></p>

<p>Applications A metabolite of Clomipramine.<br>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),<br></p>

<p>Impurity Beclomethasone Dipropionate EP Impurity L<br>Applications 1,2-Dihydro Beclomethasone Dipropionate (Beclomethasone Dipropionate EP Impurity L) is an impurity of Beclomethasone Dipropionate (B131030).<br></p>

<p>Stability Light Sensitive, Temperature Sensitive<br>Applications An oxidized derivative of the visual pigment carotenoid.<br>References Wada, A., et al.: Chem. Pharm. Bull., 56, 112 (2008), Smolensky, E., et al.: Biochem., 48, 9170 (2009),<br></p>

<p>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.<br>References Roleira, F.M., et al.: Lett. Drug. Design. Discovery., 7, 610 (2010);<br></p>

<p>Applications 4’-Hydroxyphenprocoumon is a metabolite of the oral anticoagulant Phenprocoumon (P318820).<br>References De Vries, J. et al.: J. Chrom. Biomed. Appl., 529, 479 (1990);<br></p>

<p>Applications Antihypertensive; diuretic.<br>References Piala, J.J., et al.: J. Pharmacol. Exp. Ther., 134, 273 (1961), Orzech, C.E., et al.: Anal. Profiles Drug Subs., 7, 297 (1978),<br></p>

<p>Applications Diltiazem (D460620) intermediate (impurity B).<br>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),<br></p>

<p>Applications Nonpeptide endothelin ETA receptor antagonist. Antihypertensive.<br>References Riechers, H., et al.: J. Med. Chem., 39, 2123 (1996), Billman, G.E., et al.: Curr. Opin. Invest. Drugs, 3, 1483 (2002), Vatter, H., et al.: Clin. Neuropharmacol., 26, 73 (2003),<br></p>

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

<p>Applications A metabolite of Acepromazine (A130900).<br>References Cossum, P., et al.: Drug Dispos., 9, 321 (1988), Stowell, L., et al.: J. Anal. Toxicol., 22, 166 (1998),<br></p>

<p>Applications A labelled metabolite of Spironolactone.<br>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),<br></p>

<p>Applications A non-steroidal anti-inflammatory ophthalmic agent.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Mathur, K., et al.: Bioorg. Med. Chem., 11, 1915 (2003), Zhao, M., et al.: Bioorg. Med. Chem., 15, 2815 (2007), Roy, K., et al.: Eur. J. Med. Chem., 44, 2913 (2009),<br></p>

<p>Stability Hygrscopic<br>Applications N1,N12-Diacetylspermine Dihydrochloride is a diacetylated derivative of Spermine (S680510) and is recognized as a novel tumor marker in patients with breast and colorectal cancers.<br>References Kato, M., et al.: Anticancer Res., 34, 3053 (2014); Umemori, Y., et al.: Clin. Chim. Acta, 411, 1894 (2010); Kawakita, M., et al.: J. Biochem., 139, 315 (2006); Hiramatsu, K., et al.: Clin. Cancer Res., 11, 2986 (2005)<br></p>

<p>Applications A metabolite of Quinidine.<br>References Small, D.L., et al.: J. Chem. Med., 22, 1014 (1979), Guentert, T.W., et al.: Eur. J. Drug Metab. Pharmacokinet., 7, 31 (1982), Rakhir, A., et al.: J. Pharmacokinet. Biopharm., 12, 1 (1984), Christie, D.J., et al.: J. Lab. Clin. Med., 112, 92 (1988),<br></p>

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

<p>Stability Hygroscopic, Light Sensitive, Temperature Sensitive<br>Applications Fluvastatin 3-Hydroxy-4,6-diene Sodium Salt is a metabolite of Fluvastatin (F601250), a synthetic HMG-CoA reductase inhibitor. Antilipemic.<br>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),<br></p>

<p>Applications Pipamazine is a drug od the phenothiazine class which used to be used as an antiemetic.<br>References Bhargava, K. et al.: Br. J. Pharmacol. Chemother., 22, 154 (1964); Bhargava, K. et al.: Br. J. Pharmacol. Chemother., 21, 436 (1963);<br></p>

<p>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.<br>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);<br></p>

<p>Applications Propoxyphenyl-thiohydroxyhomosildenafil is an analogue of Hydroxythiohomo Sildenafil (H963150).<br>References Balayssac, S., et. al.: J. Pharmaceut. Biomed., 63, 135 (2012)<br></p>

<p>Applications Dabigatran Carboxamide Ethyl Ester is an impurity of Dabigatran Etexilate Mesylate (D100150) which is a nonpeptide, direct thrombin inhibitor.<br>References Hauel, N., et al.: J. Med. Chem., 45, 1757 (2002); Mungall, D., et al.: Curr. Opin. Invest. Drugs, 3, 095 (2002); Stangier, J., et al.: J. Clin. Pharmacol., 45, 555 (2005)<br></p>

<p>Stability Hygroscopic<br>Applications Benfotiamine-Amide is an analog of Benfotiamine, which is a Vitamin B1 analog. Synthetic S-acyl derivative of Thiamine (T344185).<br>References Stracke, H., et al.: Exper. Clin. Endocrinol., Diabetes, 116, 600 (2008), Gohil, V., et al.: Nat., Biotechnol., 28, 249 (2010),<br></p>

<p>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).<br>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),<br></p>

<p>Applications N2'-Deacetyl-N2'-[3-(methylthio)-1-oxopropyl]-maytansine is an active metabolite of Maytansine (M197940), inhibits in vitro polymerization of tubulin and is used in the treatment of advanced breast cancer.<br>References Remillard, S., et. al.: Science, 189, 1002 (1975); Prota, A.E., et. al.: P. Natl. Acad. Sci. USA, 111, 13817 (2014)<br></p>

<p>Impurity Verapamil EP Impurity J HCl<br>Applications Nor Verapamil Hydrochloride (Verapamil EP Impurity J HCl) is a metabolite of Verapamil.<br>References Mutlib, A.E., et al.: The Journal of Pharm. &amp; Exp. Therapeutics, 252, 2, 593 (1989)<br></p>

<p>Impurity Ezetimibe Tetrahydropyran Impurity<br>Applications Ezetimibe (E975000) tetrahydropyran impurity.<br></p>

<p>Applications A metabolite of Desoxymetasone (D296970).<br>References Schriks, M., et al.: Environ. Sci. Technol., 44, 4766 (2010), Baeck, M., et al.: Eur. J. Dermatol., 20, 102 (2010), Lee, P., et al.: Bioorg. Med. Chem. Lett., 20, 69 (2010),<br></p>

<p>Applications A novel bile acid, an analogue of Cholic acid (C432600).<br>References Yamaga, N., et al.: J. Biochem., 116, 1123 (1994),<br></p>

<p>Applications Telmisartan Acyl-β-D-glucuronide is a metabolite of Telmisartan (T017000).<br>References Abe, T., et al.: J. Biol. Chem., 274, 17159 (1999), Hirano, M., et al.: Drug Metab. Dispos., 34, 1229 (2006),<br></p>

<p>Impurity Atorvastatin Pyrrolidone Analog (USP)<br>Stability Light Sensitive<br>Applications A photodegradation product of Atorvastatin (a cyclic impurity of Atorvastatin). Atorvastatin Pyrrolidone Analog (USP).<br>References Roger, D., et al.: Clin. Exp. Dermatol., 19, 88 (1994), Cosa, G., et al.: Photochem. Photobiol., 80, 159 (2004), Kerwin, B., et al.: J. Pharm. Sci., 96, 1468 (2007),<br></p>