Toxicology

<p>Applications: (R)-Apomorphine-11-sulfate Potassium Salt-d5 is the isotope labelled analog of (R)-Apomorphine-11-sulfate Potassium Salt (A727520); a derivative of (R)-Apomorphine (A727500) which is a dopamine (D1 and D2) receptor agonist, emetic, and antiparkinsonian.<br>References Neumeyer, J.L., et al.: J. Pharm. Sci., 59, 1850 (1970); Ginos, J.Z., et al.: J. Med. Chem., 18, 1194 (1975); Muhtadi, F.J., et al.: Anal. Profiles Drug Subs., 20, 121 (1991)<br></p>

<p>Stability Hygroscopic, Moisture Sensitive<br>Applications 1-​[1-​(4-​Chlorobenzoyl)​-​5-​hydroxy-​2-​methyl-​1H-​indole-​3-​acetate]β-​D-​Glucopyranuronic Acid is an analog of Indomethacin Acyl-β-D-glucuronide a metabolite of Indomethacin (I641000). Acyl glucuronides have been implicated in the toxicity of many xenobiotics and marketed drugs.<br>References Abid, A., et al.: Biochem. Pharmacol., 50, 557 (1995), Gamage, N., et al.: Toxicol. Sci., 90, 5 (2006), Cerveny, L., et al.: Drug Metab. Dispos., 35, 1032 (2007), Hayeshi, R., et al.: Eur. J. Pharm. Sci., 35, 383 (2008),<br></p>

<p>Applications Pentachloroanisole-d3 (methoxy-d3) (CAS# 1219804-52-0) is a useful isotopically labeled research compound.<br></p>

<p>Applications Loratadine (L469575) Impurity. An isomer of N-Methyl Desloratadine (M316500).<br>References Zhong, D., et al.: Pharmazie, 49, 736 (1994); Ruperez, F., et al.: J. Pharm. Biomed. Anal., 29, 35 (2002);<br></p>

<p>Applications Aldicarb Sulfone is an analog of Aldicarb (A514650) detected in agricultural products as pesticide residue.<br>References Ashby, J., et al.: Environ. Mutagen., 7, 919 (1985), Ashby, J., et al.: Mutat. Res., 257, 229 (1991), Kazius, J., et al.: J. Med. Chem., 48, 312 (2005), Benigni, R., et al.: Mutagenesis, 25, 335 (2010),<br></p>

<p>Applications (2R,5S,13aR)-2,3,4,5,7,9,13,13a-Octahydro-8-methoxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide-d2, 15N 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 Imiprothrin is an analytical standard that is also used in insect neurotoxin research.<br></p>

<p>Applications A piperidine based pesticide<br>References Iwakubo, M., et al.: Bioorg. Med. Chem., 15, 350 (2007), Jia, P., et al.: Eur. J. Med. Chem., 44, 772 (2009),<br></p>

<p>Applications A labelled metabolite of Carnitine used in diagnostic screening of patients with inherited disorders of fatty acid oxidation.<br>References Johnson, D.W. et al.: Chem. Phys. Lipids, 129, 161 (2004);<br></p>

<p>Applications Triclopyr Butotyl is a herbicide. It s very effective in reducing the canopy of honey mesquite.<br>References El-Khodary, S., et al.: Cytologia, 54, 465 (1989); Bovey, R., et al.: J. Range Management, 34, 144 (1981)<br></p>

<p>Applications Lopinavir O-Sulfate is a metabolite of Lopinavir (L469480); a selective HIV protease inhibitor and antiviral. It is a COVID19-related research product.<br>References Sham, H.L., et al.: Antimicrob. Ag. Chemother., 42, 3218 (1998); Kumar, G.N., et al.: Drug Metab. Dispos., 27, 86 (1999); Murphy, R.L., et al.: Antiviral Ther., 4, Suppl. 3, 85 (1999)<br></p>

<p>Applications Labelled Mefenamic acid metabolite.<br>References Besunder, J., et al.: Clin. Pharmacokinet., 14, 261 (1988), Smith, P., et al.: Drug Metab. Dipos., 18, 639 (1990), Kraus, D., et al.: Clin. Pharmacol. Ther., 54, 351 (1993), Sato, J., et al.: Biol. Pharm. Bull., 16, 811 (1993),<br></p>

<p>Applications 3,5-Dichloroaniline-2,4,6-d3 (CAS# 1219795-03-5) is a useful isotopically labeled research compound.<br></p>

<p>Applications Antiepileptic; Anticonvulsant that also acts as a mood stabilizer for those with bipolar disorder.<br>References Chang, Z.L., et al.: Anal. Profiles Drug Subs., 8, 529 (1979), Della Paschoa, O.E., et al.: Br. J. Pharmacol., 125, 1610 (1998), Grimes, C.A., et al.: J. Neirochem., 73, 1384 (1999), Loscher, W., Prog. Neurobiol., 58, 31 (1999),<br></p>

<p>Applications O-Desmethyl-O-ethyl Albendazole-d5 is the isotope labelled analog of O-Desmethyl-O-ethyl Albendazole (D291825); an impurity of Albendazole (A511610) which is an anthelmintic.<br>References Li, A., et al.: Zhongguo Yiyao Gongye Zazhi, 22, 360 (1991); Zhao, Y., et al.: Org. Biomol. Chem., 6, 4509 (2008); Sanderson, H., et al.: Toxicol. Lett., 187, 84 (2009)<br></p>

<p>Applications (S)-3-Aminobutan-1-ol can be used as an intermediate in the preparation of compounds having HIV integrase inhibitory activity.<br>References Johns, B. et al.: J. Med. Chem., 56, 5901 (2013);<br></p>

<p>Applications 2,6-Dimethylmorpholine is used as a reagent in the synthesis of novel 3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxylic acid amides which can exhibit antifungal activity. 2,6-Dimethylmorpholine is also used towards the synthesis of tetrahydrothiazolopyridine derivatives as potent smoothened antagonists.<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 Du, S., et al.: Molecules, 20, 8395 (2015); Du, S., et al.: Molecules, 20, 4071 (2015); Ma, H., et al.: Eur. J. Med. Chem., 89, 721 (2015)<br></p>

<p>Applications 2-Chloro-4-[(dimethylcarbamoyl)amino]benzoic Acid is a chlortoluron metabolite that was studied in transgenic tobacco plants.<br>References Shiota, N., et al.: Pestic. Biochem. Physiol., 54, 190 (1996)<br></p>

<p>Applications Bupirimate is a pyrimidine based fungicide with protective and curative activity for the control of fungal diseases by interfearing with nucleic acid synthesis.<br>References Belmonte, V. N., et al.: J. Chromatograph. A., 1264, 110 (2012); Attallah, E.R., et al.: J. Food. Agri. Envrion., 10, 755 (2012);<br></p>

<p>Applications Khellin is a compound present in the kella or picktooth fruit, used as a muscle relaxant.<br>References Shinde, P. et al.: Indian J. Nat. Prod. Res., 5, 40 (2014); Sztiller-Sikorska, M. et al.:<br></p>

<p>Impurity Levofloxacin USP Related Compound E<br>Applications Levofloxacin (L360000) impurity. A photodegradation product of Levofloxacin (L360000) in aqueous solution. Levofloxacin USP Related Compound E.<br>References Yoshida, Y., et al.: Arzneim.-Forsch., 43, 601 (1993),<br></p>

<p>Applications Protected metabolite of Mycophenolic Acid.<br>References Nelson, P., et al.: J. Med. Chem., 39, 4181 (1996), Ubukata, M., et al.: Bioorg. Med. Chem. Lett., 17, 4767 (2007),<br></p>

<p>Applications 1-Oxo Fexofenadine Methyl Ester, is an intermediate in the preparation of Fexofenadine (F322470). It can also be used for the synthesis of an oxidation metabolite of Terfenadine (T114500),a H1-receptor antagonist.<br>References Garteiz, D.A., et al.: Arzneim.-Forsch., 32, 1185 (1982), Rampe, D., et al.: Mol. Pharmacol., 44, 1240 (1993), Obradovic, T., et al.: Pharm. Res., 24, 318 (2007); Kawai, S., et al.: J. Org. Chem., 59, 2620 (1994);<br></p>

<p>Applications Azocyclotin is an organotin aracacide used in the control of mites. Azocyclotin showed weak antifeedant activity against other insects such as Spodoptera littoralis.<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 Hammann, I. et al.: Pflanzensch.-Nach., 31, 61 (1978); Ascher, K.R.S.: Naturwissenschaften, 67, 312 (1980);<br></p>

<p>Applications 2-Methylphenyl Diethylcarbamate-13C6 is an intermediate in the synthesis of o-Cresol-13C6 (C781912). Isotope labelled o-Cresol is a compound used as a disinfectant and have also been used as antiseptic in surgery.<br>References Razavi, S.M., et al.: Nat. Prod. Res., 26, 2148 (2012); Asadollahi-B. M., et al.: Environ. Toxicol. Pharmacol., 34, 826 (2012);<br></p>

<p>Applications N-Boc-3-hydroxy-L-valine is used as a reagent in the synthesis of metabolites of PPI-2458, which is a selective, irreversible inhibitor of methionine aminopeptidase-2 (MetAP2). N-Boc-3-hydroxy-L-valine is also used in the preparation of Boceprevir (B674500); an NS3 serine protease inhibitor of hepatitis C virus for the treatment of HCV infection.<br>References Arico-Muendel, C.C., et al.: Drug Metab. Dispos., 41, 814 (2013); Venkatraman, S., et al.: J. Med. Chem., 49, 6074 (2006)<br></p>

<p>Applications 4-O-Desmethyl 4-O-Ethyl Trimethoprim-D5 is a labelled analogue of 4-O-Desmethyl 4-O-Ethyl Trimethoprim (D295700).<br></p>

<p>Applications MRX-2843, is an orally available small-molecule inhibitor of both MERTK and FLT3.<br>References Minson, K. A. et al.: JCI Insight. 2016 Mar;1(3):e85630.;<br></p>

<p>Impurity Abacavir EP Impurity E<br>Applications (1R,3S)-3-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]cyclopentanemethanol (Abacavir EP Impurity E) is an impurity of Abacavir (A104990). Abacavir is a carbocyclic 2'-deoxyguanosine nucleoside reverse transcriptase inhibitor and an anti-HIV drug used to treat HIV infection (1). Intracellular enzymes convert Abacavir to its active form, carbovir-triphosphate (CBV-TP), which then selectively inhibits HIV reverse transcriptase by incorporating into viral DNA (2). Abacavir is metabolized in the liver by uridine diphosphate glucuronyltransferase and alcohol dehydrogenase resulting in inactive glucuronide and carboxylate metabolites, respectively.<br>References (1) Jackson, A., et al.: Antivir Ther. 17, 19 (2012) (2) Yuen, G. J., et al.: Clin Pharmacokinet. 47, 351 (2008)<br></p>

<p>Applications Labelled Bexarotene (B336750). Used as an antineoplastic. A selective retinoid X receptor (RXR) agonist.<br>References Boehm, M.F., et al.: J. Med. Che., 37,2930 (1994), Gottardis, M.M., et al.: Cancer Res., 56, 5566 (1996), Mukherjee, R., et al.: Nature, 386, 407 (1997), Miller, V.A., et al.: J. Clin. Oncol., 15, 790 (1997)<br></p>

<p>Applications Morphine Methylsulfonate is a derivative of Morphine (M652285), which is the principle alkaloid of opium and an analgesic used to treat both acute and chronic pain.<br>References Stefano, G., et. al.: Folia Biol, 58, 49 (2012);Buchwald, M.E., et al.: J. Pharmacol. Exp. Ther., 71, 197 (1941); Muhtadi, F.J., et al.: Anal. Profiles Drug Subs., 17, 259 (1988)<br></p>

<p>Applications Aprindine is a long-acting antiarrhythmic agent, effective when administered orally or intravenously in the treatment of ventricular arrhythmias of varying etiologies.<br>References Danilo, P. Jr., et al.: Am. Heart. J., 97, 119 (1979); Atarashi, H., et al.: Circulation. J., 66, 553 (2002);<br></p>

<p>Applications Labelled 2-Furfurylthiol Acetate (F864600). 2-Furfurylthiol Acetate is a sulfur-substituted furan derivative used as flavouring agent. 2-Furfurylthiol Acetate is a precursor to furfurylmercaptan which is very prone to oxidation to the disulfide. We will provide a detailed procedure for the preparation of the thiol from the thioacetate with spectral data upon request.<br>References Engel, K., et al.: J. Agric. Food Chem., 39, 2249 (1991), Jones, M., et al.: J. Exp. Bot., 55, 1903 (2004), Gershater, M., et al.: J. Biol. Chem., 282, 21460 (2007),<br></p>

<p>Applications Metazosulfuron is a herbicide used in paddy fields to control annual and perennial weeds.<br>References Lee, I., et. al.: The Korean Soc. Weed Sci., 31, 308 (2011)<br></p>

<p>Applications Labelled, primary metabolite of Tianeptine.<br>References Dresse, A., et al.: J. Clin. Pharmacol., 28, 1115 (1988), Grislain, L., et al.: Drug Metab. Dispos., 18, 804 (1990),<br></p>

<p>Applications Propafenone-d5 Hydrochloride is the labeled analogue of Propafenone Hydrochloride (P757500), a sodium channel blocker. Antiarrhythmic (class IC).<br>References Hollmann, M., et al.: Arzneim.-Forsch., 33, 763 (1983); Bryson, H. M., et al.:Drugs, 45, 85 (1993); Rae, A. P., et al.: Am. J. Cardiol., 82, 59N (1998)<br></p>

<p>Applications (±)-Tramadol-d6 HCl (N,N-dimethyl-d6) (cis/trans mixture) (CAS# 1189374-50-2) is a useful isotopically labeled research compound.<br></p>

<p>Applications 2-Oxo-mirabegron N-Carbamoylglucuronide is a metabolite of Mirabegron (M364900) which is a potent bladder relaxant and reagent for diabetes remedy.<br>References van Teijlingen, R., et al.: J. Chromat. B Anl. Technol. Biomed. Life Sci., 887, 102 (2012)<br></p>

<p>Applications Erythromycin Ethyl Succinate-13C,d3 is the deuterated form of Erythromycin Ethyl Succinate (E649985), which is a derivative of Erythromycin (E649950), an antibiotic.<br>References Koch, W.L., et al.: Anal. Profiles Drug Subs., 8, 157 (1979); Serisier, D. et al.: J. Am. Med. Assoc., 309, 1206 (2013);<br></p>

<p>Applications N-Arachidonoyltaurine is a polyunsaturated lipid that inhibits the Cav3.3 current in T-type calcium channels.<br>References Cazade, M., et. al.: Mol. Phearmacol., 85, 218 (2014)<br></p>