Toxicology

<p>Applications A metabolite of Sitagliptin.<br>References Beconi, M.G. , et al.: Drug Metab. Dispos., 35, 525 (2007),<br></p>

<p>Applications Acetamidine-d3 Hydrochloride is a useful compound in the synthesis of 3-​Chloro-​3-​methyl-​d3-​diazirine (CAS# 35496-73-2).<br>References Liu, M. T. H., et al.: J. Org. Chem., 45, 4515 (1980)<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 Cycloester Erythromycin Enol Ether is derived from Erythromycin A Enol Ether (E649970), which is an impurity of Erythromycin.<br>References McGuire, J.M., et al.: Antibiot. Chemother., 6, 281 (1952), Steffansen, B., et al.: Int. J. Pharm., 56, 159 (1989), Goldman, R.C., et al.: Antimicrob. Agents Chemother., 34, 1973 (1990)<br></p>

<p>Applications Trichloro[2-(chloromethyl)-2-propen-1-yl]silane is an intermediate used in the synthesis of 2-​(Chloromethyl)​allyl-​trimethylsilane (C371430), which is one of the reagents to synthesize Leucasandrolide A Macrolide (I) via Mukaiyama aldol coupling.2-​(Chloromethyl)​allyl-​trimethylsilane was used in catalytic Sakurai reaction of α,​β-​enones.<br>References Kopecky, D., et al.: J. Am. Chem. Soc., 123, 8420 (2001).Lee, P., et al.: J. Org. Chem., 66, 8646 (2001).<br></p>

<p>Applications Darunavir N-β-D-Glucuronide Sodium Salt (90%) is a salt analogue of Darunavir N-β-D-Glucuronide (D193510), which is a metabolite of Darunavir (D193500) an inhibitor of human immunodeficiency virus (HIV) protease. It is a COVID19-related research product.<br>References Vermeir, M. et al.: Drug Metab. Disp., 37, 809 (2009); Koh, Y., et al.: Antimicrob. Agents Chemother., 47, 3123 (2003); Arasteh, K., et al.: AIDS, 19, 943 (2005);<br></p>

<p>Impurity Itraconazole EP Impurity E<br>Applications trans-Itraconazole (Itraconazole EP Impurity E) is a geometrical isomer of Itraconazole (I937500). It is a COVID19-related research product.<br>References Ahn, C., et al.: J. Korean Chem. Soc., 43, 676 (1999),<br></p>

<p>Applications A labelled metabolite of Dapsone (D193250).A representative lot is 73% d8, 23% d7 and 3% d6 with no d0.<br>References Shin, I., et al.: J. App. Pharmacol., 10, 193 (2002), Bhaiya, P., et al.: Toxicol. App. Pharmacol., 215, 158 (2006), Paixao, P., et al.: Eur. J. Pharm. Sci., 36, 544 (2009),<br></p>

<p>Applications Isotope Labelled 1-Cyclopropyl-8-ethoxy-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic Acid is an impurity in the synthesis of Moxifloxacin (M745000), a fluorinated quinolone antibacterial.<br>References Woodcock, J.M., et al.: Antimicrob. Ag. Chemother., 41, 101 (1997), Stass, H., et al.: Antimicrob. Ag. Chemother., 42, 2060 (1998)<br></p>

<p>Applications Labelled trans-Hydroxy Praziquantel (H952405). The main cis-monohydroxylated metabolite of Praziquantel (P702095).<br>References Buehring, K., et al.: Eur. J. Drug Metab. Pharm., 3, 179 (1978), Moldeus, P., et al.: Methods Enzymol., 52, 60 (1978), Cioli, D., et al.: Pharmacol. Ther., 68, 35 (1995),<br></p>

<p>Applications Pipobroman-D8 is a labelled analogue of Pipobroman (P490602).<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></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 A labelled metabolite of Warfarin (W498500) in humans.<br>References Barbato, F., et al.: J. Pharm. Sci., 86, 225 (1997), Kavana, M., et al.: Biochemistry, 42, 10238 (2003), Franco, A., et al.: Environ. Toxicol. Chem., 28, 458 (2009),<br></p>

<p>Applications A metabolite of Dipyridamole.<br>References Zak, S.B., et al.: J. Pharmacol. Exp. Ther., 141, 392 (1963),<br></p>

<p>Applications Isotope labelled Diethyl Oxalate is used in the synthesis of novel indole β-diketo acid derivatives as HIV-1 integrase inhibitors.<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 Sechi, M., et al.: J. Med. Chem., 47, 5298 (2004);<br></p>

<p>Applications 7-[[(2Z)-2-(2-Amino-4-thiazolyl)-2-[(carboxymethoxy)imino]acetyl]amino]-cefixime is a cefixime impurity. Cefixime (C242800) is an orally active, third generation cephalosporin antibiotic.<br>References Kamimura, T., et al.: Antimicrob. Agents Chemother., 25, 98 (1984),Yamanaka, H., et al.: J. Antibiot., 38, 1738 (1985), Guay, D.R.P., et al.: Antimicrob. Agents Chemother., 30, 485 (1986),<br></p>

<p>Stability Moisture Sensitive, Toxic<br>Applications Benzyl Chloromethyl Ether is a reagent in the preparation of benzoyl-hydroxypyrimidine-diones, which are dual inhibitors of HIV reverse transcriptase and integrase.<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 Tang, J., et al.: Bioorg. Med. Chem. Lett., 21, 2400 (2011); Berkley, S., et al.; Nat. Med. 16, 981 (2010)<br></p>

<p>Applications N-Desdecanoyl, N-(dodeca-2,6,9-trienoyl) Daptomycin Trifluoroacetic Acid Salt is an impurity of Daptomycin (D193350), cyclic lipopeptide antibiotic derived from a fermentation product of Streptomyces roseosporus; disrupts plasma membrane function in gram-positive bacteria. Antibacterial.<br>References Allen, N.E., et al.: Antimicrob. Agents Chemother., 31, 1093 (1987), Tully, F.P., et al.: Expert Opin. Invest. Drugs, 8, 1223 (1999),<br></p>

<p>Applications Isotope labelled 1,2-Pentanediol is used in synthesizing quinoxalines from biomass-derived glycols. Also used in the synthesis of propiconazole (P770100) a fungicide as well as other antifungals.<br>References Climent, M. et al.: J. Catal., 292, 118 (2012); Zhou, Y. et al.: Carbo. Res., 344, 1289 (2009);<br></p>

<p>Applications 2,5-Thiazolylmethyl Diacarbonate is an impurity of Ritonavir (R535000), a selective HIV protease inhibitor.<br>References Daluge, S., et al.: Antimicrob. Agents Chemother., 38, 1590 (1994); Ammaranond, P., et al.: J. Clin. Virol., 26, 153 (2003); Harrigan, P., et al.: J. Infect. Dis., 191, 339 (2005); Miller, J., et al.: Bioorg. Med. Chem. Lett., 16, 1788 (2006); Koppala, S., et al.: J. Chromatogr. Sci., 53, 662 (2015);<br></p>

<p>Stability Temperature Sensitive<br>Applications Antibiotic A21 is a new polyene macrolide Amphotericin amide antibiotic with antimycotic effectiveness.<br>References Flores-Romero, J. D., et al.: Org. Process Res. Dev., 20, 1529 (2016), Antillon, A., et al.: PLoS One, 11, 9 (2016)<br></p>

<p>Applications N-Hydroxy-methyl Methoxy Tenofovir Alfenamide is an impurity of Tenofovir (T018500) which is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor. It is used as an anti-HIV agent. Antiviral.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997); Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007);<br></p>

<p>Applications 2-(Bromomethyl)-5-(trifluoromethyl)furan is an intermediate used to prepare tertiary sulfonamides as liver X receptor antagonists. It is also used to synthesize hydantoin based inhibitors of MMP13 with potential use in osteoarthritis.<br>References Zuercher, W., et al.: J. Med. Chem., 53, 3412 (2010); De Savi, C., et al.: Bioorg. Med. Chem. Lett., 23, 4705 (2013)<br></p>

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

<p>Applications 2,4'-Dibromobenzophenone (CAS# 78281-59-1) is a useful research chemical compound.<br></p>

<p>Applications Daptomycin Impurity B1-1 is an impurity of Daptomycin (D193350), cyclic lipopeptide antibiotic derived from a fermentation product of Streptomyces roseosporus; disrupts plasma membrane function in gram-positive bacteria. Antibacterial.<br>References Allen, N.E., et al.: Antimicrob. Agents Chemother., 31, 1093 (1987), Tully, F.P., et al.: Expert Opin. Invest. Drugs, 8, 1223 (1999),<br></p>

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

<p>Applications A di-substituted cyclohexane carboxylic acids used in the synthesis of macrolide antibiotics.<br>References Goss, R.J. et al.: Org. Biomol. Chem., 4, 5071 (2006);<br></p>

<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 Fenoxaprop<br></p>

<p>Applications n-Nonanoic-9,9,9-d3 acid is labelled n-Nonanoic Acid (N649385) which is commonly used in conjunction with glyphosate, a non-selective herbicide, for a quick burn-down effect in the control of weeds in turfgrass. It is also used in the preparation of plasticizers and lacquers.<br>References Pline, W., et al.: Weed Technol., 14, 667 (2000); Frade, J., et al.: Anal. Bioanal. Chem., 395, 2167 (2009)<br></p>

<p>Applications α-Chloro-p-methyltoluene-13C is the labeled analogue of α-Chloro-p-methyltoluene(C369770). α-Chloro-p-methyltoluene is a building block that has been used as a reactant for the preparation of 6-aminoquinolone derivatives as submicromolar hepatitis C virus NS5B inhibitors<br>References Manfroni, G., et. al.: J. Med. Chem., Ahead of Print (2013)<br></p>