Derivati delle Purine e Pirimidine

<p>Applications 7-Cl-kynurenic acid (7-Cl-KYNA) is a potent, selective antagonist of the NMDA/glycine receptor but penetrates poorly through the blood-brain barrier.  Its prodrug, L-4-Cl-kynurenine (4-Cl-KYN), readily enters the brain from the circulation and provides antiexcitotoxic neuroprotection after systemic application.<br>References Leeson, P., et al.: J. Med. Chem., 37, 4053 (1994), Hilmas, C., et al.: J. Neurosci., 2001, 21, 7463 (2001), Palmer, G., et al.: Curr. Drug Targets, 2, 241 (2001), Wu, H., et al.: Exp. Neurol., 177, 222 (2002),<br></p>

<p>Applications Hydroxymethyl Sumatriptan is an analog of Sumatriptan (S810000), a serotonin 5HT1-receptor agonist.<br>References Humphrey, P.P.A., et al.: Brit. J. Pharmacol., 94, 1123 (1988), Doenicke, A., et al.: Lancet 1, 1309 (1988),<br></p>

<p>Stability Hygroscopic<br>Applications Tenofovir Disoproxil derivative as antiviral and antitumor agent.<br></p>

<p>Stability Light Sensitive, Temperature Sensitive, Very Hygroscopic<br>Applications Tenofovir Monoisoproxil Dimer Ammonium Sodium Salt is an impurity in the synthesis of Tenofovir disoproxil (T018505),an acyclic phosphonate nucleotide analogue; reverse transcriptase inhibitor.<br>References Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007),<br></p>

<p>Rizatriptan (Risatriptan) is a selective 5-hydroxytryptamine 1B/1D receptor agonist used in the study of migraine.</p>

<p>Stability Moisture sensitive<br>Applications Chloromethyl Isopropyl Carbonate is an antiviral agent and a Tenofovir (T018500) intermediate. Tenofovir is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor used as an anti-HIV agent.<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 Mackman, R., et al.: Bioorg. Med. Chem., 15, 5519 (2007), Baudy, R., et al.: J. Med. Chem., 52, 771 (2009),<br></p>

<p>Applications A Nicotinic acid (N429250) derivative for treatment of hypercholesterolemia and hyperlipidemia and cardiovascular disease.<br>References Hales, N.J., et al.: J. Med. Chem., 36, 3853 (1993),<br></p>

<p>Impurity Temozolomide USP Related Compound A<br>Applications Temozolomide USP Related Compound A<br></p>

<p>Applications A nicotinic acid derivative which shows a dopaminergic neurotoxicity.<br>References Rollema, H., et al.: J. Med. Chem., 33, 2221 (1990),<br></p>

<p>Xanthine, a purine breakdown product, is turned into uric acid by xanthine oxidase and blocks adenosine receptors.</p>

<p>Applications Nicotinic Acid-13C6 is labelled Nicotinic acid. It is a precursor of the coenzymes NAD and NADP. Widely distributed in nature; appreciable amounts are found in liver , fish, yeast and cereal grains. Dietary deficiency is associated with pellagra. The term “niacin” has also been applied to nicotinamide or to other derivatives exhibiting the biological activity of nicotinic acid. Vitamin (enzyme cofactor).<br>References Darby, W.J., et al.: Nutr. Rev., 33, 289 (1975), Black, A., et al.: Eur. J. Clin. Nutr., 54, 395 (2000), Cole, T., et al.: Br. Med. J., 320, 1240 (2000), Forshee, R., et al.: J. Nutr., 134, 2733 (2004),<br></p>

<p>Applications Caffeine-d3 (1-methyl-d3) (CAS# 26351-03-1) is a useful isotopically labeled research compound.<br></p>

<p>Stability Hygroscopic<br>Applications It is a potent and selective inhibitor of bacterial dihydrofolate reductase, the enzyme responsible for the NADPH-dependent reduction of 7,8-dihydrofolate to 5,6,7,8-tetrahydrofolate. Antibacterial.This compound is a contaminant of emerging concern (CECs).<br>References Manius, G.J., et al.: Anal. Profiles Drug Subs., 7, 445 (1978), Roth, B., et al.: J. Med. Chem., 23, 379 (1980), Brogden, R.N., et al.: Drugs, 23, 405 (1982),<br></p>

<p>Applications Guanidinoacetic Acid is an important marker for renal failure, in kidney transplantation, and for the renal metabolic activity.<br>References Zugno, A., et al.: Neurochem. Res., 33, 1804 (2008), Debray, F., et al.: Neurol., 71, 44 (2008), da Silva, R., et al.: Am. J. Physiol., 296, E256 (2009),<br></p>

<p>Applications Labelled Urea. Physiological regulator of nitrogen excretion in mammals; synthesized in the liver as an end-product of protein catabolism and excreted in urine. Also occurs normally in skin. Emollient; diuretic.<br>References Demetriou, A., et al.: Science, 233, 1190 (1986), Aebischer, P., et al.: Nat. Med., 2, 696 (1996), Prakash, S., et al.: Biotechnol. Bioeng., 46, 621 (1995),<br></p>

<p>Applications Succinimide is a reagent that is used in the synthesis of Lumiflavin (L473900), which is a toxic photolysis product of vitamin B2 (R415000).<br>References Zhao, X. et al.: Chemosphere, 63, 1116 (2006); Litke, S.V. et al.: Khim. Fiz., 10, 48 (1991); Ye, W. et al.: Guang. Yaox. Xueb., 12, 175 (1996);<br></p>

<p>Applications A well-known, highly active stimulant of cell divisions in plant tissue cultures.<br>References D.S. Letham: Phytochemistry, 12, 2445 (1973)<br></p>

<p>Applications Uric Acid is a heterocyclcic compound that is created when purine nucleotides are broken down of by the human body. High blood concetration of Uric Acid is known as hyperuricemia and is often associated with a wide range of disorders and medical conditions such as gout, diabetes and metabolic syndrome. Uric acid may be a marker of oxidative stress and may have a potential therapeutic role as an antioxidant.<br>References Heinig, M. et al.: Cle. Clin. J. Med., 73, 1059 (2006); Glantzounis, G.K. et al.: Curr. Pharmac. Des., 11, 4145 (2005); Dehghan, A. et al.: Diab. Care, 31, 361 (2008); Nakagawa, T. et al.: Am. J. Physiol. Renal Physiol., 290, F625 (2006);<br></p>

<p>Applications 9-(2-Propenyl)adenine is an N-substituted purine used in the preparation of mesityl dihydroisoxazolyl homo-N-nucleosides.<br>References Thalassitis, A. et al.: Bioorg. Med. Chem. Lett., 19, 6433 (2009); Chiacchio, U. et al.: Tetrahedron, 60, 441 (2004)<br></p>

<p>Applications Acyclic phosphonate nucleotide analogue; reverse transcriptase inhibitor. 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 Caffeine-13C3 is a labelled analogue of Caffeine (C080100), a bitter, white crystalline xanthine alkaloid that acts as a stimulant drug and a reversible acetylcholinesterase inhibitor. Caffeine is found in varying quantities in the seeds, leaves, and fruit of some plants, where it acts as a natural pesticide that paralyzes and kills certain insects feeding on the plants. In humans, caffeine acts as a central nervous system stimulant, temporarily warding off drowsiness and restoring alertness. Caffeine is a cardiac and respiratory stimulant; diuretic. Caffeine is toxic at sufficiently high doses.A study at Johns Hopkins University indicates that caffeine can improve pattern separation memory.<br>References Zubair, U.M., et al.: Anal. Profiles Drug Subs., 15, 71 (1986); Cherrah, Y., et al.: Biochem. Pharmacol., 37, 1311 (1988);  Chem. and Eng. News p.34, Jan. 20, (2014)<br></p>

<p>Applications CAL-101 is a PI3K/mTOR pathway inhibitor used in the treatment of myeloid leukemia through sensitizing the cells to combatting drugs. Potent PI3K-p110-delta inhibitor.<br>References Airiau, K. et al.: Cell. Death. Dis., 4, e827 (2013); Kulesz-Martin, M. et al Canc. Biol. Ther., 14m 95 (2013);<br></p>

<p>Applications 2-[3-Carboxy-4-(2-methylpropoxy)phenyl]-4-methyl-5-thiazolecarboxylic Acid is an impurity of Febuxostat (F229000), an xanthine oxidase/ xanthine dehydrogenase inhibitor used for the treatment of hyperuricemia and chronic gout.<br>References Kadivar, M.H.,e t al.: J. Pharm. Biomed. Anal., 56, 749 (2011);<br></p>

<p>Applications Tenofovir Alafenamide Fumarate is a prodrug of Tenofovir (T018500), which is a reverse transcriptase inhibitor used to treat HIV and Hepatitis B. 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 Allopurinol-13C,15N2, is the labeled analogue of Allopurinol (A547300), acting as an Xanthine oxidase inhibitor, and used in treatment of hyperuricemia and chronic gout.<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 Benezra, S.A., et al.: Anal. Profiles Drug Subs., 7, 1, (1978), Dalbeth, N., et al.: Rheumatology, 44, 1090 (2005), Dinarello, C., et al.: J. Exp. Med., 201, 1355 (2005),<br></p>

<p>Applications Methotrexate Dimethylamide is an impurity of Methotrexate (M260675) which is a folic acid antagonist. Used as a antineoplastic and antirheumatic.<br>References Freeman, M.V., J. Pharmacol. Exp. Ther., 122, 154 (1958), Weinblass, M.E., et al.: N. Engl. J. Med., 312, 818 (1985),<br></p>

<p>Stability Hygroscopic<br>Applications Tenofovir Alafenamide is a prodrug of Tenofovir (T018500), which is a reverse transcriptase inhibitor used to treat HIV and Hepatitis B. 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 Metabolite of Theophylline and Caffeine.<br>References Yu, Ch. et al.: J. Bacteriol. 191, 4624 (2009); Geraets, L. et al.: Biochem. Pharmacol. 72, 902 (2006).<br></p>

<p>Applications Labelled precursor in the biosynthesis of Biopterin. First isolated from the pupae of bees.<br>References Kobashi, I., et al.: Agric. Biol. Chem., 35, 47 (1971), Fukushima, S., et al.: J. Biol. Chem., 247, 4549 (1972),<br></p>

<p>Impurity Methotrexate EP Impurity D<br>Applications N10-Methyl Pteroic Acid (Methotrexate EP Impurity D) is a Methotrexate (M260675) impurity D.<br>References Cramer, S., et al.: Cancer Res. 1984, 44, 1843 (1984), Hendel, J., et al.: Eur. J. Clin. Pharmacol., 26, 103 (1984),<br></p>

<p>Stability Very Hygroscopic<br>Applications Tri-POC Tenofovir Dimer is a dimer of Tenofovir Disoproxil (T018505), an acyclic phosphonate nucleotide analogue; reverse transcriptase inhibitor. Used as an anti-HIV agent. Antiviral. It is also used in the preparation of phosphocitrate for the treatment of rheumatoid and osteoarthritis in the elderly.<br>References Turhanen, P. et al.: J. Org. Chem., 72, 1468 (2007);<br></p>

<p>Applications N-Acetyl Memantine is an intermediate used for preparation of Memantine (M218000).<br>References Gerzon, K., et al.: J. Med. Chem., 6, 760 (1963), Reddy, J., et al.: Org. Process Res. Dev., 11, 268 (2007),<br></p>

<p>Applications Ethyl 2-(4-Hydroxyphenyl)-4-methylthiazole-5-carboxylate is used in the synthesis of the major metabolites of Febuxostat (F229000), a xanthine oxidase/xanthine dehydrogenase inhibitor. Used for treatment of hyperuricemia and chronic gout. 40-120 mg/day febuxostat was proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.<br>References Li, X., et. al.: Lett. Org. Chem., 12, 217 (2015); Vallu, V., et. al.: Anal. Chem. Indian J., 14, 339 (2014); Osada, Y., et al.: Eur. J. Pharmacol., 241, 183 (1993); Okamoto, K., et al.: J. Biol. Chem., 278, 1848 (2003); Mayer, M.D., et al.: Am. J. Therap., 12, 22 (2005); Tomlinson, B., et al.: Curr. Opin. Invest. Drugs, 6, 1168 (2005)<br></p>

<p>Impurity Ondansetron EP Impurity D; Ondansetron USP Related Compound D<br>Applications 1,2,3,9-Tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one (Ondansetron EP Impurity D; Ondansetron USP Related Compound D) is an impurity of Ondansetron (O655000).<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 Feng, R. et al.: Zhong. Yaox. Zaz., 46, 1436 (2011); Zizkovsky, V. et al.: J. Pharm. Biomed. Anal., 44, 1048 (2007)<br></p>

<p>Applications (R)-9-[2-(Hydroxypropyl] Adenine (Desphosphoryl Tenofovir) (cas# 14047-28-0) is a useful reagent for preparing the antiviral drug tenofovir.<br>References Dietz, J.-P., et al.: ChemRxiv, 1 (2020)<br></p>

<p>Impurity Allopurinol EP Impurity C / Allopurinol USP Related Compound C<br>Applications 3-(4H-1,2,4-Triazol-4-yl)-1H-pyrazole-4-carboxamide (Allopurinol EP Impurity C) is an impurity of Allopurinol (A547300).<br></p>

<p>Applications Ondansetron is a specific serotonin (5-HT3) receptor antagonist. Antiemetic.<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 Kris, M.G., et al.: J. Clin. Oncol., 6, 659 (1988); Faris, P..L., et al.: Lances, 355, 792 (2000)<br></p>

<p>Impurity Ondansetron EP Impurity A/ Ondansetron USP Related Compound A<br>Applications 3-[(Dimethylamino)methyl]-1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (Ondansetron EP Impurity A) is an impurity of Ondansetron (O655000), an antiemetic.<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 Mackinnon, J.W.M., et al.: Eur. J. Cancer Clin. Oncol., 25, 61 (1989);<br></p>

<p>Stability Hygroscopic<br>Applications The indole acetic acid metabolite of Zolmitriptan (Z639000) formed by human hepatocytes.<br>References Wild, M.J. et al.: Xenobiotica, 29, 847 (1999);<br></p>

<p>Applications Thyroxine is one of the thyroid hormones involved in the maintenance of metabolic homeostasis. Synthesized and stored as amino acid residues of thyroglobulin, the major protein component of the thyroid follicular colloid. Synthesis and secretion are regulated by the pituitary hormone (TSH). Deiodinated in peripheral tissues to the active metabolite, liothyronine. The D-form has very little activity as a thyroid hormone, but has been used to treat hyperlipidemia.<br>References Post, A., et al.: Anal. Profiles Drug Subs., 5, 225 (1976); Nelson, J.C., et al.: Clin. Chem., 34, 1737 (1988); Fischer, D.A., et al.: Clin. Chem., 42, 135 (1996); Cavalieri, R.R., et al.: Thyroid, 7, 177 (1997);<br></p>

<p>Applications A fluorescent analog of Nicotinamide Adenine Dinucleotide as a coenzyme for glutamate dehydrogenase.<br>References Gafni, A., et al.: Biochemistry, 20, 6041 (1981), Creedon, K., et al.: J. Biol. Chem., 269, 16364 (1994), Seley, K., et al.: Bioorg. Med. Chem., 6, 797 (1998),<br></p>

<p>Applications Lablled Caffeine (C080100). Caffeine is a bitter, white crystalline xanthine alkaloid that acts as a stimulant drug and a reversible acetylcholinesterase inhibitor. Caffeine is found in varying quantities in the seeds, leaves, and fruit of some plants, where it acts as a natural pesticide that paralyzes and kills certain insects feeding on the plants. In humans, caffeine acts as a central nervous system stimulant, temporarily warding off drowsiness and restoring alertness. Caffeine is a cardiac and respiratory stimulant; diuretic. Caffeine is toxic at sufficiently high doses.<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 Zubair, U.M., et al.: Anal. Profiles Drug Subs., 15, 71 (1986); Cherrah, Y., et al.: Biochem. Pharmacol., 37, 1311 (1988);<br></p>

<p>Stability Hygroscopic<br>Applications Precursor in the biosynthesis of Biopterin. First isolated from the pupae of bees.<br>References Kobashi, I., et al.: Agric. Biol. Chem., 35, 47 (1971), Fukushima, S., et al.: J. Biol. Chem., 247, 4549 (1972),<br></p>

<p>Applications (S)-Tenofovir is an S-enatiomeric derivative of Tenofovir (T018500). (S)-Tenofovir displays virucidal activity against herpes, visna virus and retrovirus. The S enantiomer of Tenofovir (T018500) is less effective against HIV than their (R)-enantiomeric counterparts.<br>References Balzarini, J. et al: Biochem. Biophys. Res. Comm., 219, 337 (1996); Balzarini, J. et al.: Antimicrob. Agents. Ch., 37, 332 (1993); Thormar, H. et al.: Antimicorb. Agents. Ch., 37, 2540 (1993)<br></p>

<p>Applications 1-Bromo-3,5-dimethyladamantane (cas# 941-37-7) is a compound useful in organic synthesis.<br></p>

<p>Applications Labelled Febuxostat (F229000). Xanthine oxidase/xanthine dehydrogenase inhibitor. Used for treatment of hyperuricemia and chronic gout.<br>References Osada, Y., et al.: Eur. J. Pharmacol., 241, 183 (1993), Okamoto, K., et al.: J. Biol. Chem., 278, 1848 (2003), Mayer, M.D., et al.: Am. J. Therap., 12, 22 (2005), Tomlinson, B., et al.: Curr. Opin. Invest. Drugs, 6, 1168 (2005),<br></p>

<p>Applications 8-Descarboxamido-8-cyano Temozolomide is a useful synthetic intermediate in the synthesis of Temozolomide (T017775); an imidazotetrazine alkylating agent and antineoplastic.<br>References Newlands, E.S., et al.: Cancer Treat. Rev., 23, 35 (1997); Kim, C., et al.: J. Biol. Chem., 274, 1233 (1999); Hait, W., et al.: Cancer Res., 69, 1263 (2009); Wang, Y., et al.: J. Org. Chem., 62, 7288 (1997)<br></p>

<p>Applications 2-Fluoroadenosine is a fluorinated analog of Adenoside (A280400) nucleotide.<br>References Long, X., et al.: J. Pharmacol. Exper. Ther., 335, 781 (2010); Ham, M., et al.: J. Pharmacol. Exper. Ther., 335, 607 (2010);<br></p>

<p>Applications Methotrexate α-tert-Butyl Ester is an intermediate to the synthesis of folic acid antagonist Methotrexate (M260675) used in the study of membrane-associated folate transporters from L1210 cells.<br>References Yoshii, T., et al.: J. Am. Chem. Soc., 136, 16635 (2014);<br></p>