Dérivés des Purines et Pyrimidines

<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>Stability Hygroscopic<br>Applications Methotrexate Hexaglutamate is a metabolite of Methotrexate (M260675); a folic acid antagonist, 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 rac-Clopidogrel Carboxylic Acid Hydrochloride is a salt metabolite of rac-Clopidogrel.<br></p>

<p>Applications 2-Chloro-6-amino-9-(2’,3’,5’-tri-O-acetyl-β-D-ribofuranosyl)purine (cas# 79999-39-6) is a compound useful in organic synthesis.<br></p>

<p>Applications 3-Descyano Febuxostat Ethyl Ester is an impurity 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 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>Applications 4-Hydroxy-1,3-benzenedicarbonitrile is used in the preparation of febuxostat (F229000), a non-purine xanthine oxidase inhibitor used as a treatment for hyperuricaemia and chronic gout.<br>References Smith, C.J., et al.: Bioorg. Med. Chem. Lett., 20, 346 (2010); Cramp. S., et al.: BIoorg. Med. Chem. Lett., 20, 2516 (2010); Sato, T., et al.: Bioorg. Med. Chem. Lett., 19, 184 (2009);<br></p>

<p>Stability Very Very Moisture sensitive<br>Applications Chloroformic Acid Chloromethyl Ester is used as a reagent in the synthesis of carbamates and carbonates.<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 Safadi, M. et al.: Pharm. Res. 10, 1350 (1993); Loren, J.C. et al.: Synlett, 18, 2847 (2005);<br></p>

<p>Applications A nicotinic acid derivative for prevention and treatment of cancer by activating RUNX3 gene.<br>References Ludwig, et al.: Cancer Res., 50, 2470 (1990), Gupta., et al.: Biomed. Environ. Sci., 13,122 (2000), Cai., et al.: J. Med. Chem., 46, 2474 (2003),<br></p>

<p>Stability Photosensitive<br>Applications It is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML).<br></p>

<p>Stability Hygroscopic<br>Applications Methotrexate intermediate.<br>References Feng, Y., et al.: J. Med. Chem., 49, 770 (2006),<br></p>

<p>Stability Hygroscopic, Temperature Sensitive<br>Applications 4-[2-(4-Chlorobutylidene)hydrazinyl]-N-methylbenzenemethanesulfonamide is an intermediate in the synthesis of 3-(2-Aminoethyl)-N-methyl-1H-indole-5-methanesulfonamide (Didesmethyl Sumatriptan) (Sumatriptan EP Impurity E) (A609165), which is an antimigraine agent. A Sumatriptan intermediate.<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 This compound is an isomer of compound (E925685) used in the synthesis of neuraminidase inhibitors.<br>References Jarinrat K. et al.: Bioorg. Med. Chem. Lett., 20, 2152 (2012);<br></p>

<p>Applications A metabolite of Tetrabenazine in vivo, which is likely the active pharmacological agent. The cis isomer of Dihydrotetrabenazine is used for the treatment of hyperkinetic movement disorders.<br>References Kilbourn, M., et al.: Eur. J. Pharmacol., 278, 249 (1995), Perera, R., et al.: J. Med. Chem., 46, 2599 (2003), Mager, D., et al.: J. Pharm. Sci., 94, 2475 (2005), Zheng, G., et al.: Bioorg. Med. Chem., 16, 5018 (2006),<br></p>

<p>Stability Hygroscopic<br>Applications Tenofovir (T018500) impurity.<br></p>

<p>Applications Caffeine-D10 is the labeled compound of Caffeine(C080100). Caffeine (Pentoxifylline EP Impurity F) is a bitter, white crystalline xanthine alkaloid that acts as a stimulant drug and a reversible acetylcholinesterase inhibitor (1,2,3). 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. Caffeine is a non-competitive inhibitor of acetylcholinesterase (3).<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>Applications Barbituric Acid (B118650) derivative with anti-convulsive properties. Controlled Substance.<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 Carissime, M. et al.: Farmac. Edi. Sci., 17, 390 (1962); Harvey, D.J. et al.: Drug. Metab. Disp., 5, 527 (1977);<br></p>

<p>Applications Methotrexate Tetraglutamate is a metabolite of Methotrexate (M260675); a folic acid antagonist, 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>Applications Degradation product of Sumatriptan Succinate (S810000).<br>References Xu, X. et al.: J. Pharmaceut. Biomed. 367, 26 (2001)<br></p>

<p>Applications Labelled Hydroxyurea. An anti-neoplastic - inhibits ribonucleoside reductase and DNA replication. A potential therapy for sickle cell anemia which involves the nitrosylation of sickle cell hemoglobin. Horseradish peroxidase catalyzes nitric oxide formation from hydroxyurea in the presence of hydrogen peroxide.<br>References Ratcliffe, W., et al.: Lancet, 339, 164 (1992), Roodman, G., et al.: Cancer, 80, 1557 (1997), Horwitz, M., et al.: J. Clin. Endocrinol. Metab., 2003, 88, 1603 (2003),<br></p>

<p>Applications (+)-9-deMe-DTBZ is a desmethyl derivative of Tetrabenzine (T284000), a dopamine depleting agent. An antidyskinetic; antipsychotic.<br>References Schwartz, et al.: Biochem. Pharmacol., 15, 645 (1966), Janovic, J., et al.: Ann. Neurol., 11, 41 (1982), Janovic, J., et al.: Neurology, 38, 391 (1988),<br></p>

<p>Applications 6-Oxo-(S,S)-Palonosetron is an impurity of (S,S)-Palonosetron (P165800), a serotonin 5-HT3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). Antiemetic.<br>References Clark, R.D., et al.: J. Med. Chem., 36, 2645 (1993), Wong, E.H.F., et al.: Br. J. Pharmacol., 114, 851 (1995), Grunberg, S.M., et al.: Expert. Opin. Pharmacother., 4, 2297 (2003), Eisenberg, P., et al.: Ann. Oncol., 15, 330 (2004), Siddiqui, M.A.A., et al.: Drugs, 64, 1125 (2004),<br></p>

<p>Applications 2-Pyrimidinemethanamine (cas# 75985-45-4) is a useful research chemical.<br></p>

<p>Stability Light Sensitive, Temperature Sensitive<br>Applications 1-Methyl-1,4-dihydronicotinamide (cas# 17750-23-1) is a compound useful in organic synthesis.<br></p>

<p>Applications A metabolite of Febuxostat (F229000), a novel nonpurine selective inhibitor of Xanthin Oxidase.<br>References Grabowski, B., et al.: J. Clin. Pharmacol., 51, 189 (2011); 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 Valbenzine is a highly selective vesicular monoamine transporter 2 inhibitor. It is used in the treatment of tardive dykinesia.<br>References O'Brien, C. et al.: Movement Dis., 30, 1681 (2015);<br></p>

<p>Applications Benzofuran-6-carboxylic Acid is a reagent in the development of potent LFA-1/ICAM antagonist SAR 118 as an opthalmic solution for treating dry eyes. Preparation of piperidinylpyrimidine derivatives as inhibitors of HIV-1 LTR activation.<br>References Zhong, M., et al.: ACS Med. Chem., 3, 203 (2012); Fujiwara, N., et al.: Bioorg. Med. Chem., 16, 9804 (2008)<br></p>

<p>Applications 5-Carboxy-2'-deoxyuridine, is a derivative of Trifluridine, an anti-herpesvirus antiviral drug, used primarily on the eye.<br>References Kuster, P., et al.: CLAO J. 24(2), 122 (1998); O’Brien, W., Invest. Opthalmol. Vis. Sci., 32 (9), 2455 (1991);<br></p>

<p>Applications An impurity of Tenofovir (T018500(P)). Tenofovir 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-Hydroxy-N-(pyridin-4-yl)butanamide is a useful synthetic intermediate.<br></p>

<p>Applications Diethyl p-Toluenesulfonyloxymethylphosphonate 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>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 Febuxostat 67M-2 is a derivative compound of Febuxostat 67M-1 (F229005) which is an inhibitor of xanthine oxidase. It reduces uric acid production in the body and also used to reduce the risk of gout or kidney stone formation.<br>References Du, J., et al.: Handbook of Metabolic Pathways of Xenobiotics, 4, 1395 (2014)<br></p>

<p>Applications 8-13C-Uric Acid is the labeled analogue of Uric Acid (U829200), 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 Ethyl 2-(4-Butoxy-3-cyanophenyl)-4-methylthiazole-5-carboxylate, is an impurity in the synthesis of Febuxostat n-Butyl Isomer (F229035).<br></p>

<p>Stability Very Hygroscopic<br>Applications Tenofovir Dimer is a dimer of Tenofovir (T018500). Tenofovir is a reverse transcriptase inhibitor. Used as an anti-HIV agent.<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>Impurity Proguanil USP Related Compound E (1-(4-chlorophenyl)-3-cyanoguanidine)<br>Applications Halo-aryl substituted guanidine derivative used in the preparation of antimalarial agents. Proguanil USP Related Compound E (1-(4-chlorophenyl)-3-cyanoguanidine).<br>References Warner, V. et al.: J. Pharmac. Sci., 66, 418 (1977); Das, A. et al.: Ind. Drugs, 20, 19 (1980);<br></p>

<p>Applications Tenofovir is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor. It is used as an anti-HIV agent. Antiviral. Tenofovir (T018500) impurity.<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 An impurity of the antiviral drug Oseltamivir (O700100). It is a COVID19-related research product.<br></p>

<p>Impurity Naratriptan Impurity F<br>Stability Hygroscopic<br>Applications 4-[1,5-Bis-(2-methylsulfamoylethyl)-1H-indol-3-yl]-1-methylpyridinium Chloride is an impurity of Naratriptan (N378730).<br></p>