Toxicología

<p>Applications 4’-epi-Entecavir-di-o-benzyl ether is an impurity of Entecavir (E558900) which is an oral antiviral drug used in the treatment of hepatitis B infection.<br>References Honkoop, P., et al.: Expert Opin. Invest. Drugs, 12, 683 (2003), Chang, T.-T., et al.: N. Engl. J. Med., 354, 1001 (2006),<br></p>

<p>Applications rac-Deacetamide Linezolid Phthalimide is a possible intermediate of Linezolid (L466500) which inhibits bacterial mRNA translation.<br>References Brickner, S.J., et al.: J. Med. Chem., 39, 673 (1996); Ford, C.W., et al.: Antimicrob. Agents Chemother., 40, 1508 (1996); Rybak, M.J., et al.: Pharmacotherapy, 18, 456 (1998); Stevens, D.L., et al.: Clin. Infect. Dis., 34, 1481 (2002)<br></p>

<p>Applications An active insecticidal constituent of pyrethrum flowers. Oxidizes rapidly and becomes inactive in presence of air.<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 Okey, A., et al.: Pharmacol. Ther., 45, 241 (1990), Barter, R., et al.: Toxicol. Appl. Pharmacol., 113, 36 (1992), Hood, A., et al.: Toxicol. Sci., 49, 263 (1999),<br></p>

<p>Applications Methyl 2-((((Benzyloxy)carbonyl)amino)methyl)-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxylate is an intermediate used in the synthesis of N-((5-Hydroxy-6-oxo-4-((2,4,6-trifluorobenzyl)carbamoyl)-1,6-dihydropyrimidin-2-yl)methyl)-1,3,4-oxadiazole-2-carboxamide (H950690), which is a derivative of Raltegravir (R100305), a potent integrase (IN) inhibitor for WT and S217Q PFV IN.<br>References Hare, S., et al.: Proc. Natl. Acad. Sci. U. S. A., 107, 20057 (2010); Hicks, C., et al.: Clin. Infect. Dis., 48, 931 (2009); Moss, D., et al.: Antimicrob. Agents Chemother., 56, 3020 (2012); Hare, S., et al.: Mol. Pharmacol., 80, 565 (2011)<br></p>

<p>Applications Amoxycilloic Acid Trimer is an impurity of Amoxycilloic Acid (A634265); a degradation product/impurity of Amoxicillin (A634235, 3H2O) which is a semi-synthetic antibiotic related to Penicillin and an antibacterial.<br>References Connor, S., et al.: J. Pharm. Pharmacol., 46, 128 (1994); Van G., et al.: J. Vet. Pharmacol. Ther., 26, 139 (2003); Brogden, R.N., et al.: Drugs, 18, 169 (1979); Bird, A.E., et al.: Anal. Profiles Drug Subs. Excip., 23, 1 (1994)<br></p>

<p>Applications Malonic Acid-2-13C is labelled Malonic Acid (M158005) which is a small bioactive molecule, that can be used in variuos reactions. It is the classic example of a competitive inhibitor, which acts against succinate dehydrogenase (complex II) in the respiratory electron transport chain.<br>References Weiner, N., "Malonic acid", Org. Synth.; Coll. Vol. 2: 376;<br></p>

<p>Applications Inhibits FGF-induced angiogenesis. Inhibits replication of human immunodeficiency virus type 1. Teratogenic sedative. There is now a growing clinical interest in Thalidomide, and it is introduced as an immunomodulatory agent used primarily in combination with dexamethasone to treat multiple myeloma.<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 D’Amato, r.J., et al.: Proc. Natl. Acad. Sci. USA, 91, 4082 (1994), Makonkawkeyoon, S., et al.: Proc. Natl. Acad. Sci. USA, 90, 5974 (1993), Schumacher, H., et al.: J. Pharmacol. Exp. Therap., 160, 189 (1968)<br></p>

<p>Applications Estradiol 6-N3-Adenine is a depurinating adduct that is created by the interaction of specific metabolites of estrogens in the body with DNA. Unfortunately, these adducts are endogeneous initiators of various human cancers, such as breast &amp; prostate.<br>References Yang, L., et al.: Prostate, 69, 41 (2009); Zahid, M., et al.: Chem. Res. Toxicol., 19, 164 (2006); Zhang, Y., et al.: Metabol. Clin. Exp., 56, 887 (2007)<br></p>

<p>Applications N-(4-(4-(4-(((2R,4S)-2-((1H-1,2,4-Triazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)phenyl)hydrazinecarboxamide is an intermediate in the synthesis of derivatives of Itraconazole (I937500), an orally active antimycotic and antifungal compound.<br>References Heeres, J., et al.: J. Med. Chem., 27. 894 (1984);<br></p>

<p>Applications 1-Chloro-2-(α-chlorophenylmethyl)benzene-d5 is the isotope labelled analog of 1-Chloro-2-(α-chlorophenylmethyl)benzene (C427570); a reagent in the synthesis of bifonazole analogs which have antibacterial and antifungal activities. It is also used in the preparation of diphenylpiperazine N-type calcium channel inhibitors.<br>References El Hage, S., et al.: Arch. Pharm., 344, 402 (2011); Pajouhesh, H., et al.: Bioorg. Med. Chem. Lett., 20, 1378 (2010)<br></p>

<p>Applications A Cobicistat (C633150) impurity. Cobicistat is a HIV protease inhibitor and have been coadministered with low-dose ritonavir (R535000) as a pharmacoenhancer, significantly increasing their plasma concentrations.<br>References Von, H., Exp. Rev. Clin. Pharmacol., 5, 557 (2012); Lepist, E.I., et al.: Antimicrob. Agent. Chemother., 56, 5409 (2012); Orr, S.T.M., et al.: J. Med. Chem., 55, 4896 (2012);<br></p>

<p>Applications Clindamycin 3-Palmitate Hydrochloride, is an impurity in the synthesis of Clindamycin Palmitate Hydrochloride (C580035), a semi-synthetic antibiotic with high bioavailability. Clindamycin Palmitate is an antibacterial.<br>References Bharathi, Ch. et al.: J. Pharm. Biomed. Anal., 48, 1211 (2008); Platzer, D., et al.: J. Pharm. Biomed. Anal., 41, 84 (2006);<br></p>

<p>Stability Hygroscopic<br>Applications Raloxifene 6-Glucuronide Lithium Salt is A metabolite of Raloxifene (R100000), a nonsteroidal estrogen receptor mixed agonist/antagonist.<br>References Dodge, J., et al.: Bioorg. Med. Chem. Lett., 7, 993 (1997); Jeong, E., et al.: Drug Metab. Dispos., 33, 785 (2005); Trontelj, J., et al.: Pharmacol. Res., 52, 334 (2005); Oswald, S., et al.: Clin. Pharmacol. Ther., 79 206 (2006)<br></p>

<p>Applications A Nicotine metabolite. Carcinogen.<br></p>

<p>Applications 8-Hydroxy Efavirenz is a metabolite of Efavirenz (E425000), a nonnucleoside HIV-1 reverse transcriptase inhibitor.<br>References Gorski, J., et al.: Biochem. Pharmacol., 47, 1643 (1994), Desta, Z., et al.: J. Pharmacol. Exp. Ther., 285, 428 (1998), Langmann, P., et al.: Eur. J. Med. Res., 7, 309(2002), Chang, T., et al.: Drug Metab. Dispos., 31, 7 (2003),<br></p>

<p>Applications p-Chloro-N,N-diethylaniline-d10 is derived from 4-Chlorophenylamine (C421894), which is an organic chemical reagent and precursor in the synthesis of various drugs and dyestuffs. It is a building block and degradation product of Chlorhexidine (C335045), an antiseptic as well as azo dyes and pigments in printing and textiles.<br>References Leucea, D. et al.: Ind. Text., 61, 304 (2010); Below, H. et al.: Microchim. Acta 146, 129 (2004);<br></p>

<p>Applications Diethyl 2-(methylthio)-4,5-pyrimidinedicarboxylate<br></p>

<p>Applications Contact herbicide used also to produce desiccation and defoliation.<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 Brian, et al.: Nature, 181, 446 (1958), Gaines, T.B., et al.: Fundam. Appl. Toxicol., 7, 299 (1986),<br></p>

<p>Applications 5-cis-Tetradecenoyl-d3 Carnitine is labelled 5-cis-Tetradecenoyl Carnitine (T291425) which is one of the metabolites found in the lymph fluid collected from dietary stressed rats.<br>References Ardawi, M., et al.: Biochem. J., 212, 835 (1983), Otton, R., et al.: J. Endocrinol., 174, 55 (2002), Gu, H., et al.: Anal. Chem., 79, 89 (2007),<br></p>

<p>Applications 3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxylic Acid (cas# 176969-34-9) is a useful research chemical.<br></p>

<p>Applications 7-Methyltryptophol is a metabolite of Tryptophan (T947200), an essential amino acid.<br>References Liu, F., et al.: Bioorg. Med. Chem., 18, 4167 (2010), Kumar, R., et al.: Eur. J. Med. Chem., 45, 2265 (2010), Cai, W., et al.: Bioorg. Med. Chem., 18, 1899 (2010),<br></p>

<p>Applications An antitussive. Controlled substance (opium derivative).<br>References Kabayashi, S., et al.: Arzneim.-Forsch., 20, 43 (1970), Yanagita, T., et al.: Bull. Narc., 29, 33 (1977),<br></p>

<p>Applications 3-trans-Hydroxy Norcotinine (cas# 1292911-83-1) is a compound useful in organic synthesis.<br></p>

<p>Applications Fluoxetine (F597100) derivative. A stereoselective inhibitor of serotonin re-uptake and phosphodiesterase. Potential antidepressants<br>References Cashman, J. et al.: Bioorgan Med. Chem. 17, 337 (2009)<br></p>

<p>Applications Tiafenacil is a uracil herbicide used as a pesticide for the prevention and control of plants.<br>References Peng, X., et al. Faming Zhuanli Shenqing, 68pp Patent 2018 CODEN:CNXXEV<br></p>

<p>Applications 10β-Hydroxyl Dextrorphan 3-O-β-D-Glucuronide is a metabolite of Dextrorphan.<br>References Thurman, E. Michael., et al.: J. Chrom. A., 1259, 158-166 (2012)<br></p>

<p>Applications 3,5,6-Trichloro-8-quinolinecarboxylic Acid is an impurity of Quinclorac (Q670300), which is a disubstituted quinolinecarboxylic acid that is part of a new class of highly selective auxin herbicides. Quinclorac is used in rice to control dicotyledonous and monocotyledonous weeds, particularly barnyardgrass (Echinochloa crus-galli). Quinclorac is also used for weed control in turfgrasses.<br>References Haden, E. et al.: Proc. Br. Corp. Prot. Conf. Weeds, 1, 77 (1985); Chism, W.J. et al.: Weed Sci., 39, 62 (1991); Grossmann, K. et al.: Weed Sci., 46, 707 (1998);<br></p>

<p>Applications Testosterone 17-Hexahydrobenzoate-d11 is the isotope analog of Testosterone 17-Hexahydrobenzoate. Testosterone 17-Hexahydrobenzoate is a metabolite of testosterone (T155000), which is used in biological studies to determine the hemolytic and lipophilic activity of this anabolic steroid.<br>References Biagi, G.L., et al.: J. Med. Chem., 13, 944 (1970); Biagi, G. L., et al.: J. Med. Chem., 18, 873 (1975)<br></p>

<p>Applications Labelled Famotidine. Histamine H2-receptor antagonist. Antiulcerative.<br>References Takeda, M., et al.: Arzneim.-Forsch., 32, 734 (1982), Miwa, M., et al.: J. Clin. Pharmacol. Ther. Toxicol., 22, 214 (1984), Takabatke, T., et al.: Eur. J. Clin. Pharmacol., 28, 327 (1985),<br></p>

<p>Applications 1-(2,2-Dihydroxyethyl)-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic Acid is an intermediate in the synthesis of Bictegravir-15N, d2 (B382096), which is the labeled version of Bictegravir, which is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.<br>References Tsiang M. et al.: Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097;<br></p>

<p>Applications (Z)-rac-Luliconazole is a stereoisomer of Luliconazole (L473770) which is an azole antifungal drug.<br>References Uhida, K., et al.: J. Infect. Chemother., 10, 216 (2004); Niwano, ., et al.: Antimicro. Agents Chemother., 42, 967 (1998)<br></p>

<p>Stability Light Sensitive<br>Applications Rifabutin Impurity C is an impurity of Rifabutin (R505000), a semisynthetic derivative of Rifamycin S that inhibits nucleic acid synthesis.<br>References O’Brien, R.J., et al.: Infect. Dis., 9, 519 (1987), Anand, R., et al.: Antimicrob. AG. Chemother., 32 (684 (1988), Skinner, M.H., et al.: Antimicrob. Agent Chemother., 33, 1237 (1989),<br></p>

<p>Impurity Valganociclovir EP Impurity J<br>Applications Ganciclovir Mono-O-propionate is a potential prodrug of Ganciclovir (G235000). Ganciclovir Mono-O-propionate was also found to exhibit anti-viral activity through experimental studies.<br>References Dias, C.S., et al.: J. Pharma. Sci., 91, 660 (2002);<br></p>

<p>Applications 2-Ethoxy-4-ethoxysulfonylbenzoic Acid is a derivative of Methyl 2-Ethoxybenzoate (M220113), a useful chemical reagent, used in the synthesis and antibacterial triazoles and oxadiazoles, as well as sulfonamide compounds.<br>References Shi, Z. et al.: Compt. Rend. Chim., 18, 1320 (2015);<br></p>

<p>Applications Verazide is derived from Isoniazid (I821450), which is an antibiotic for treatment of Mycobacterium tuberculosis, inhibits mycolic acid biosynthesis. Metabolized by hepatic N-acetyltransferase (NAT) and cytochrome P450 2E1 (CYP2E1) to form hepatotoxins. Selectively induces expression of CYP2E1. Reversibly inhibits CYP2C19 and CYP3A4 activities, and mechanistically inactivates CYP1A2, CYP2A6, CYP2C19 and CYP3A4 at clinically relevant concentrations. Antibacterial (tuberculostatic).<br>References Brewer, G.A., et al.: Anal. Profiles Drug Subs., 6, 183 (1977), Weber, W.W., et al.: Clin. Pharmacokinet., 4, 401 (1979)<br></p>