Miscellaneous Organic Molecules with Isotopical Substitutions

Applications Labelled analogue of Dibenz[a,h]anthracene, a polycyclic aromatic hydrocarbon (PAH) and a known carcinogen. Dibenz[a,h]anthracene has produced positive results in bacterial DNA damage and mutagenicity assays and in mammalian cell DNA damage, mutagenicity and cell transformation assays. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Farmer, P.B. et al.: Mutat. Res. Re. Mutat. Res., 544, 397 (2003); Leadon, S. et al.: Carcinogenesis, 16, 3021 (1995); Andrews, A.W. et al.: Mutat. Res., 51, 311 (1978); Kaden, D.A. et al.: Cancer Res., 39, 4152 (1979);

Stability Hygroscopic Applications A nitrofuran labelled antibiotic with low resistance potential that is rapidly metabolized by mammals. Active against both Gram-positive and Gram-negative bacteria. Nitrofurantoin is also a prooxidant that is cytotoxic due to the generation of intracellular H2O2. Antibacterial.Environmental contaminants; Food contaminants; Heat processing contaminants References Cadwallader, D.E., et al.: Anal. Profiles Drug Subs., 5, 345 (1976), Rogers, R.G., et al.: Am. J. Obstr. Gynecol., 191, 182 (2004),

Applications A novel labelled HIV reverse transcriptase inhibitor useful in treatment of HIV infection. References Scholler-Gyure, M., et al.: J. Clin. Pharmacol., 48, 322 (2008), Thakur, A., et al.: Eur. J. Med. Chem., 43, 471 (2008),

Applications Labelled analogue of Glycine (G615990), a non-essential amino acid for human development. Glycine (G615990) is an inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors. References Scott, D., et al.: J. Neurosci., 21, 3063 (2001), Laube, B., et al.: Neuropharmacology, 47, 994 (2004), Papadakis, M., et al.: J. Biol. Chem., 279, 14703 (2004), Chen, P., et al.: Mol. Pharmacol., 67, 1470 (2005), Wolosker, H., et al.: Mol. Neurobiol., 36, 152 (2007),

Applications An amino acid isolated from Cholera vibrio. References Windsor, et al.: J. Biol. Chem., 192, 595 (1951), Scott, A.I., et al.: Synth. Commun., 10, 127 (1980),

Applications Labelled Carbaryl (C175895). Cholinesterase inhibitor. Ectoparasiticide. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Chauzat, M., et al.: Env. Entomol., 38, 514 (2009), Raut, P., et al.: Pestol., 33, 21 (2009), Henseler, R., et al.: Toxicol., 261, 9 (2009), Banerjee, K., et al.: J. Agric. Food Chem., 57, 4068 (2009),

Applications Cholesterol-3,4-13C2 (CAS# 78887-48-6) is a useful isotopically labeled research compound.

Applications alpha-Methylstyrene-d10 (CAS# 10362-82-0) is a useful isotopically labeled research compound.

Applications Bictegravir-15N, d2 is the labeled version of Bictegravir, which is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM. References Tsiang M. et al.: Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097;

Applications Deuterated Zolpidem, a selective non-benzodiazepine GABAA receptor agonist. Sedative, hypnotic. Controlled substance (depresssant). References Arbilla, S., et al.: Arch. Pharmacol., 330, 248 (1985), Cashman, J.N., et al.: Brit. J. Clin. Pharmacol., 21, 205 (1986)

Applications Isotope labelled Triethyl Phosphate is a useful synthetic intermediate. It was used in the synthesis of mesoporous spheres of metal oxides and phosphates. It was also used to prepare α,β-unsatd. tricyclic enones via an intramolecular Horner-Wadsworth-Emmons cyclization. Phosphorus Flame Retardant. References Dong, A., et al.: J. Am. Chem. Soc., 125, 4976 (2003); Pace, V., et al.: Tetrahedron Lett., 50, 3050 (2009)

Stability Hygroscopic Applications 3,4-Dihydroxyphenylacetic Acid-d5 is the labeled analogue of 3,4-Dihydroxyphenylacetic Acid (D454250), a metabolite of Dopamine (D533782). References Johnson, S. et al.: J. Physiol., 450, 455 (1992)

Applications A CNS stimulant. Anorexic. In attention deficit disorder with hyperactivity. Controlled substance (stimulant). Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Lands, M., et al.: J. Pharmacol. Exp. Ther., 89, 382 (1947), Repke, D.B., et al.: J. Pharm. Sci., 67, 1167 (1978), Pope, H.G., et al.: J. Clin. Psychiatry, 47, 339 (1986), Cho, A.K., et al.: Science, 249, 631 (1990),

Applications The major metabolite of the Cinchona alkaloid Quinidine. 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),

Applications Testosterone 17-Decanoate-d3, is the labeled analogue of Testosterone 17-Decanoate (T155120), an ester of Testosterone (T155000). Testosterone 17-Decanoate, can be used as a potential long-acting male contraceptive, with the combination of subcutaneous etonogestrel implants. References Brady, B. M., et al.: Human Reproduction, 21 (1), 285 (2006); Themmen, A., et al.: Endocr. Rev. 21, 551 (2000);

Applications Labelled D-Glucose is a simple sugar that is present in plants. A monosaccharide that may exist in open chain or cyclic conformation if in solution. It plays a vital role in photosynthesis and fuels the energy required for cellular respiration. D-Glucose is used in various metabolic processes including enzymic synthesis of cyclohexyl-α and β-D-glucosides. Can also be used as a diagnostic tool in detection of type 2 diabetes mellitus and potentially Huntington's disease through analysis of blood-glucose in type 1 diabetes mellitus. References Wang, R., et al.: J. Mol. Catal. B. Enz., 56, 131 (2009); Springhorn, C. et al.: J. Clin. Endocrinol. Metab., 97, 4640 (2012); Hashimoto, K. et al.: J. Clin. Endocrinol. Metab., 97, 3016 (2012); Avelange, M. et al.: Plant. Phys., 94, 1157 (1990); Cramer, C. et al.: J. Chem. Soc., 115, 5745 (1993);

Stability Hygroscopic Applications (+)-Isolysergic Acid Diethylamide-d10 is labelled iso-LSD (I821060) which is an inactive diastereomer of the illicit psychedelic drug LSD, a potent hallucinogen and non-selective serotonin receptor agonist. References Hoffer, et al.: Clin. Pharmacol. Ther., 6, 183 (1965), Keller, U., et al.: Biochemistry, 27, 6164 (1988), Mey, G., et al.: Mol. Microbiol., 46, 305 (2002), Steiner, U., et al.: Planta, 224, 533 (2006),

Applications Glucocorticoid receptor binding.A representative lots showed approximately 10% d8. References Gazdar, A., et al.: Cancer Res., 50, 5488, (1990), Bird, I., et al.: Endocrinology, 134, 2468 (1994), Auchus, R., et al.: J. Biol. Chem., 273, 3158 (1998), Dardis, A., et al.: J. Endocrinol., 179, 131 (2003),

Applications Norfloxacin-d5 is deuterium labeled Norfloxacin (N681000), a synthetic fluoroquinolone and an antibacterial agent. Norfloxacin can be used to treat urinary tract infections. References Koga, H., et al.: J. Med. Chem., 23, 1358 (1980), Hirai, K., et al.: Antimicrob. Agents Chemother., 19, 188 (1981), Holmes, B., et al.: Drugs, 30, 482 (1985),

Stability Hygroscopic Applications Labelled Fluoxastrobin (F596700). Leaf-systemic broad-spectrum fungicide for use in cereal and food crops; member of methoxy-imiodihydro-dioxazines. Agricultural fungicide. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Milus, E., et al.: Plant Dis., 78, 697 (1994), D'Mello, J., et al.: Eur. J. Plant Pathol., 104, 745 (1998), Domijan, A., et al.: Food Addit. Contam., 22, 677 (2005),

Applications L-Glutaryl Carnitine-d6 Chloride is the isotope labelled analog of L-Glutaryl Carnitine (G597600) and a metabolite of L-Carnitine (C184110). References Millington, D., et al.: J. Inherit. Metab. Dis., 13, 321 (1990), Chace, D., et al.: Clin. Chem., 49, 1797 (2003),

Applications Synergistic insecticidal and acaricidal organophosphorus compound. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Applications 1,10-Decanedioic-d16 Acid (CAS# 73351-71-0) is a useful isotopically labelled compound for studying saturated fatty acids. References Yamada, T., et al.: Adv. Synth. Catal., 358, 3277 (2016)

Applications 5-Oxo-DL-proline-d5 is a labelled cyclized derivative of L-Glutamic Acid (G596960). The pyroglutamate core has potential application for synthesis of novel anti-bacterials. References Mischo A. et al.: ChemBioChem., 13, 1421 (2012); Angelov P. et al.: Org. Biomol. Chem.: 10, 3472 (2012);

Applications Influenza viral neuraminidase inhibitor; structural analog of the sialic acid. Antiviral. References Woods, J.M., et al.: Antimicrob. Agents Chemother., 37, 1473 (1993), Pegg, M.S., et al.: Biochem. Mol. Biol. Int., 32, 851 (1994), Monto, A.S., et al.: J. Am. Med. Assoc., 282, 31 (1999),

Applications N-Methyl-d3-pyrrole (cas# 20687-13-2) is a compound useful in organic synthesis. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Applications Labelled analogue of Bisdemethoxycurcumin, one of the three major forms of curcuminoids found in the rhizomes of turmeric. Bisdemethoxycurcumin displays antioxidant, anti-inflammatory as well as chemotherapeutic activity. Bisdemethoxycurcumin acts as an inhibitor of human pancreatic α-amylase, a target for type-2 diabetes . References Ponnusamy, S. et al.: Food Chem., 135, 2638 (2012); Hung, C.-M. et al.: J. Agric. Food. Chem., 60, 8427 (2012); Jayaprakasha, G.K. et al.: Food Chem., 98, 720 (2006);

Applications Resorcinol-d4, is the isotope labelled analog of Resorcinol (R144700). Resorcinol is a benzene derivative used as keratolytic and antiseborrheic. Also used in veterinary medicine as a topical antipruritic and antiseptic (has been used as intestinal antiseptic). Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Strakosch, E.A. et al.: Arch. Dermat. Syphil., 48, 393 (1943); Dyson, G.M.: Pharm. J., 120, 582 (1928); Sabalitschka, T. et al.: Pharmazeutiche Zeitung, 81, 335 (1936);

Applications This is a controlled substance (depressant). Anticonvulsant; sedative; hypnotic. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Goldenthal, E.I., et al.: Toxicol. Appl. Pharmacol., 18, 185 (1971), Chao, M.K.C., et al.: Anal. Profiles Drug Subs., 7, 359 (1978),

Stability Hygroscopic Applications Labelled Serotonin (S274980). Serotonin is a monoamine neurotransmitter. References Kuraishi, Y., et al.: Biol. Pharm. Bull., 31, 2143 (2008); Morera, E., et al.: Bioorg. Med. Chem. Lett., 19, 6806 (2009); Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010);

Applications Labelled specific opioid antagonist. Narcotic antagonist. References Jasinski, D.R., et al.: J. Pharmacol. Exp. Ther., 157, 420 (1967), McNicholas, L.F., et al.: Drugs, 27, 81 (1984), Hasson, M.M.A., et al.: Anal. Profiles Drug Subs., 14, 453 (1985), Stowe, C., et al.: Ann. Pharmacother., 27, 447 (1993),

Stability Hygroscopic Applications Labelled Gemcitabine, an antineoplastic. References Hertel, L.W., et al.: Cancer Res., 50, 4417 (1990), Abbruzzese, J.L., et al.: J. Clin. Oncol., 9, 491 (1991), Ruiz, V.W.T., et al.: Biochem. Pharmacol., 46, 762 (1993),