Toxicology

<p>Applications Elagolix Sodium is a novel uracil phenylethylamine that acts as potent human gonadotropin-​releasing hormone receptor (hGnRH-​R) antagonist.<br>References Chen, C. et al.: J. Med. Chem., 51, 7478 (2008);<br></p>

<p>Applications A tobacco smoke-derived nitrosamine which is activated by multiple human cytochrome P 450s including the polymorphic human cytochrome P 4502D6.<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 Castonguay, A., et al.: Cancer Lett., 46, 93 (1989), Crespi, C.L., et al.: Carcinogenesis, 12, 1197 (1991),<br></p>

<p>Impurity Pilocarpine Hydrochloride EP Impurity B<br>Stability Hygroscopic<br>Applications Pilocarpic Acid Sodium Salt is an imidazole derivative used in the preparation of novel sequentially labile pilocarpine prodrugs for improved ocular delivery.<br>References Bungaard, H. et al.: J. Med. Chem., 28, 978 (1985); Jarvinen, T.e t al.: Int. J. Pharmac., 79, 233 (1992);<br></p>

<p>Impurity Fluconazole EP Impurity D<br>Applications 2-Desfluoro Fluconazole (Fluconazole EP Impurity D) is an impurity of the antifungal agent Fluconazole (F421000).<br>References Ramesh, B. et al.: J. Pharm. Res., 4, 1401 (2011); Al-Rimawi, F.: Jor. J. Chem., 4, 357 (2009);<br></p>

<p>Applications A protected metabolite of the fluorinated quinolone antibacterial Ciprofloxacin.<br></p>

<p>Impurity Ampicillin EP Impurity A ; Amoxicillin USP Related Compound A<br>Applications (+)-6-Aminopenicillanic Acid (Amoxicillin EP Impurity A) is the core structure in penicillins, obtained from the fermentation brew of the Penicillium mold. (+)-6-Aminopenicillanic Acid is used as the main starting block for the preparation of numerous semisynthetic penicillins.<br>References Zel'tser, I.Z. et al.: Gig. Truda Prof. Zabol., 5, 59 (1983); Hamilton-Miller, J.M.T.: Int. J. Antimicrob. Agents, 31, 189 (2008); Novikova, N.D. et al.: Mikol. Fitopatol., 7, 101 (1973);<br></p>

<p>Applications A metabolite of methylmalonic acid and propionic acid in children with methylmalonic acid and propionic acid metabolic disorders.<br>References Duran, M., et al.: Clin. Chimica Acta, 82, 93 (1978), Thompson, G.N., et al.: Pediatric Res., 27, 413 (1990),<br></p>

<p>Applications Derivative of thyroxine. Antilipemic.<br>References Banz, H., et al.: Fortschr. Med., 97, 1942 (1979),<br></p>

<p>Applications: N,N'-Di(2-hydroxybenzyl)ethylenediamine-N,N'-diacetic Acid Monohydrochloride Hydrate is a component for treating or preventing obesity and insulin resistance and mitrochondrial-associated disorders.N,N'-Di(2-hydroxybenzyl)ethylenediamine-N,N'-diacetic Acid Monohydrochloride Hydrate is also the monohydrochloride hydrate of HBED (H107503), which is an iron chelator useful in treating iron overload.<br>References Milburn, Michael, WO 2007008548, (2007)Bergeron, Raymond J., WO 9939706, (1999)<br></p>

<p>Applications Chloramphenicol Succinate Sodium is a derivative of Chloramphenicol (C325030) which are broad spectrum antibiotic obtained from cultures of the soil bacterium Streptomyces venezuelae. It has a broad spectrum of activity against Gram-positive and gram-negative bacteria. Antibacterial; antirickettsial.<br>References Bartz, et al.: J. Biol. Chem., et al.: 172, 445 (1948), Gottlieb, et al.: J. Bacteriol., 55, 409 (1948), Szulczewski, D., et al.: Anal. Profiles Drug Subs., 4, 47 (1975), Price, A., et al.: J. Antibiot., 43, 118 (1981), Shalit, I., et al.: Drugs, 28, 281 (1984),<br></p>

<p>Applications Amphotericin B Methyl Ester is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B Methyl Esterin is a cholesterol binding compound that showed inhibiton of human immunodeficiency virus type 1 (HIV-1).<br>References Waheed, A.A. et al.: J. Biol. Chem., 281, 28699 (2006); Waheed, A. et al.: J. Virol., 82, 9776 (2008); Waheed, A., et al.: J. Biol. Chem., 281, 28699 (2006)<br></p>

<p>Stability Hygroscopic<br>Applications Cefixime EP Impurity B Acetic Acid Salt is an impurity of the third generation cephalosporin antibiotic, Cefixime (C242800).<br>References Bian, L. et al.: Yao. Fen. Zaz., 30, 872 (2010);<br></p>

<p>Applications Intermediate used in the synthesis of a variety of antibacterial and antifungal activities of symmetric and asymmetric azines.<br>References Veena, K., et al.: E-J.Chem, 8, 354 (2011),<br></p>

<p>Applications rac Efavirenz is a mixture of both enantiomers for Efavirenz (E425000), a nonnucleoside HIV-1 reverse transcriptase inhibitor. Antiviral.<br>References Young, S.D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995); Hadaruga, D. et al.: J. Med Chem., 48, 2432 (2005);<br></p>

<p>Applications 1-Chloro-2-(α-chlorophenylmethyl)benzene is used as 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 Ombitasvir is a pharmaceutical drug that is used in the treatment of hepatitis C virus in patients with HCV genotype 1 infection. It inhibits an important viral phosphoprotein, NS5A, which is involved in viral replication, assembly, and secretion.<br>References Feld, J.J., et al.: New Eng. J. Med., 370, 1594 (2014); Lawitz, E., et al.: J. Hepatol., 57, 24 (2012); Afdhal, N., et al.: New England J. Med., 370, 1889 (2014)<br></p>

<p>Applications Episterol is a compound influencing ergosterol biosynthesis, and thus acting as an antifungal agent.<br>References Mallory, J. et al.: Pharmacol., 3, 179 (2012); Mueller, C. et al.: Steroids, 78, 483 (2013);<br></p>

<p>Applications Sinigrine, is a glucosinolate which is found naturally in Cruciferae including the genus Brassica. When enzymatically hydrolysed, Sinigrine yields isothiocyanates and give a pungent taste. Both Sinigrine, and isothiocyanates, have been shown to have anticancer activity as well as antifungal and antibacterial properties.<br>References Cools, K., et al.: J. Chromatograohy B., 901, 115 (2012); Okullcz, M., et al.: Materiae Veg., 65 (3), 217 2010;<br></p>

<p>Applications Mangiferin is a xanthonoid, a chemical compound found in mangoes and in Anemarrhena asphodeloides rhizomes. Mangiferin has effect of hepatinica and choleretic, and is used to therapy hepatitis. Mangiferin is an anti-inflammatory, antivirotic, central nervous system inhibit function and immunologic suppression. Mangiferin has curative effect on chronic bronchitis. Mangiferin has cytotoxicity effect on hepatocellularcarcinoma ce1l, and may induce apoptosis. Mangiferin has the effect of antioxidation and delaying caducity.<br>References Tawab, M., et al.; Drug Metab. Dispos., 31, 1065 (2003), Yim, J., et al.: Biol. Pharm. Bull., 27, 1580 (2004), Kim, Y., et al.: J. Microbiol. Biotechnol., 18, 1109 (2008), Joh, E., et al.: Biochem. Pharmacol., 82, 278 (2011),<br></p>

<p>Applications N-Formyl Erythromycin A is a derivative of Erythromycin (E649950), an antibiotic medication.<br>References Koch, W.L., et al.: Anal. Profiles Drug Subs., 8, 157 (1979),<br></p>

<p>Applications (R)-(+)-2-Amino-3-benzyloxy-1-propanol is used as a reagent to synthesize beta-amino alcohols, compounds that are used as therapeutic agents to treat heart disease. (R)-(+)-2-Amino-3-benzyloxy-1-propanol is also used as a reagent to synthesize 15-membered macrolide antibiotics, drugs that are used to treat respiratory tract infections.<br>References Fisher, G., et al.: J. Org. Chem., 60, 2026 (1995); Metro, T., et al.: J. Org. Chem., 72, 6556 (2007); Sugimoto, T., et al.: Bioorg. Med. Chem., 20, 5787 (2012)<br></p>

<p>Impurity Salmeterol EP Impurity B<br>Applications A novel antibacterial analog of the antibacterial drug Sulfamethoxazole (S699086).<br></p>

<p>Impurity Azithromycin Related Compound O<br>Applications Azithromycin N-Ethyl is an analogue of Azithromycin (A927000), an semi-synthetic macrolide antibiotic that is related to Erythromycin (E649950).<br>References Bright, G.M., et al.: J. Antibio., 41, 1029 (1988);<br></p>

<p>Applications A metabolite of Lamivudine (L172500).<br>References Soudeyns, H., et al.: Antimicrob. Agents Chemother., 35, 1386 (1991), Denapoli, L., et al.: Nucleosides Nucleotides, 12, 21 (1993),<br></p>

<p>Applications PSI-6130 is an experimental treatment for hepatitis C. PSI-6130 is a member of a class of antiviral drugs known as nucleoside polymerase inhibitors. PSI-6130 inhibits the hepatitis C virus RNA dependant RNA polymerase called NS5B.<br>References Clark, J., et al.: J. Med. Chem., 48, 5504 (2005); Stuyver, L., et al.: Antiviral Chem. Chem., 17, 79 (2006)<br></p>

<p>Applications Succinylacetone (SA) is a specific marker for the inherited metabolic disease, hepatorenal tyrosinemia. It was developed a stable-isotope for the determination of SA in dried blood spots (DBS) and liquid urine using a 13C4-SA as internal standard. The method was applied retrospectively and prospectively for the diagnosis of hepatorenal tyrosinemia and for follow-up of patients under treatment.<br>References Kvittingen, E., et al.: Inher. Metab. Dis., 14, 554 (1991), Lindstedt, S., et al.: Lancet, 340, 813 (1992), Schulze, A., et al.: Clin. Chem., 47, 1424 (2001), Allard, P., et al.: Clin. Biochem., 37, 1010 (2004),<br></p>

<p>Applications 4'-Dimethylamino 7,8-Dihydroxyflavone is a synthetic 7,8-Dihydroxyflavone derivative which promotes neurogenesis and exhibits potent antidepressant effect. The 7,8-dihydroxy groups are essential for the agonistic effect. 4'-Dimethylamino 7,8-Dihydroxyflavone displays higher TrkB agonistic activity than that of 7,8-Dihydroxyflavone (D452830).<br>References Thoenen, H., et al.: Trends Neurosci., 14, 165 (1991); Nibuya, M., et al.: J. Neurosci., 15, 7539 (1995); Kaplan, D., et al.: Curr. Opin. Neurobiol., 10, 381 (2000); Saarelainen, T., et al.: J. Neurosci., 2003, 23, 349 (2003);<br></p>

<p>Applications Mebutizide is a thiazide diuretic.<br>References Madrid A.J. et al.: Rev. Clin. Esp., 114, 143 (1969);<br></p>

<p>Applications A metabolite of the fluorinated quinolone antibacterial Ciprofloxacin.<br></p>

<p>Applications Clindamycin Palmitate is a semi-synthetic antibiotic with high bioavailability. Clindamycin Palmitate is an antibacterial.<br>References Platzer, D., et al.: J. Pharm. Biomed. Anal., 41, 84 (2006),<br></p>

<p>Applications 5,6-Dihydroyangonin is a derivative of Yangonin (Y100550), a lactone isolated from the Kava plant (Piper methysticum). 5,6-Dihydroyangonin was shown to exhibit potential antibacterial and antifungal activities.<br>References Keledjian, J., et al.: J. Pharm. Sci., 77, 1003 (1988), Clouatre, D., et al.: Toxicol. Lett., 150, 85 (2004), Mathews, J., et al.: Drug Metab. Dispos., 33, 1555 (2005), Clayton, N., et al.: Exp. Toxicol. Pathol., 58, 223 (2007),<br></p>

<p>Stability Hygroscopic<br>Applications Piperacillin sodium is an antibiotic related to penicillin. Also, it possesses anti-microbial activity against enterobacteria.<br>References Zhang, Y., et al.: Linchuang Wuzhen Wuzhi, 27, 63-65 (2014)<br></p>

<p>Applications 4-(4-(4-(4H-1,2,4-Triazol-4-yl)phenyl)piperazin-1-yl)phenyl Acetate is an intermediate in the synthesis of Deoxo Anhydro Itraconazole Bromide (D231675). Deoxo Anhydro Itraconazole Bromide is an impurity of Itraconazole (I937500), which is orally active antimycotic drug structurally related to Ketoconazole (K186000). Antifungal.<br>References Espinel-Ingroff, A., et al.: Antimicrob. Agents Chemother., 26, 5 (1984); Heykants, J., et al.: Mycoses, 32, Suppl 1, 67 (1989); Sugar, A.M.,et al.: Curr. Clin. Top. Infect. Dis., 13, 74 (1993)<br></p>

<p>Applications 3-(7-Cyano-5-(2-nitropropyl)indolin-1-yl)propyl Benzoate is used in the preparation of Silodosin (S465000), an α1a-adrenoceptor antagonist. It is used in treatment of benign prostatic hypertophy.<br>References Shibata, K., et al.: Mol. Pharmacol., 48, 250 (1995); Murata, S., et al.: J. Urol., 164, 578 (2000)<br></p>

<p>Impurity Mometasone Furoate EP Impurity A<br>Applications Mometasone Furoate Impurity A (Mometasone EP Impurity A) is an impurity of Mometasone Furoate, a topical corticosteroid used as an anti-inflammatory.<br>References Shapiro, E.L., et al.: J. Med. Chem., 30, 1581 (1987); Graft, D., et al.: J. Allergy Clin. Immunol., 98, 724 (1996)<br></p>

<p>Applications Lamivudine epimer.<br>References Chang, C., et al.: J. Biol. Chem., 267, 13938 (1992), Jeong, L., et al.: J. Med. Chem., 36, 181 (1993),<br></p>

<p>Stability Hygroscopic<br>Applications A pro-drug of Ganciclovir. Used in treatment of retro-virus.<br>References Acosta, E., et al.: Clin. Pharmacol. Ther., 81, 867 (2007), Nassetta, L., et al.: J. Antimicrob. Chemother., 63, 862 (2009),<br></p>

<p>Applications 2-Amino-4-chlorobenzoic Acid is used in the preparation of quinazolinone derivatives observed to be useful in the treatment of Alzheimer’s disease. Also it aids in the synthesis of non-nucleoside, thumb pocket 2 HCV NS5B polymerase inhibitors used in Hepatitis C therapy.<br>References Stammers, T. et al.: Bioorg, Med, Chem. Lett., 23, 2585 (2013);<br></p>