Autres

<p>Applications A labelled metabolite of Diazepam; it had a much weaker anticonvulsant effect.<br>References Hara, T., et al.: J. Med. Chem., 21, 263 (1978),<br></p>

<p>Applications Palbociclib-d4 is an isotope labelled compound of Palbociclib (P139900). Palbociclib (P139900) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.<br>References Finn, R., et al.: Breast Cancer Res., 11, 5 (2009)<br></p>

<p>Applications Zaleplon Formide is an impurity of Zaleplon (Z145000), a selective non-benzodiazepine GABAA receptor agonist.<br>References Radl, S., et al.: J. Heterocycl. Chem, 47, 276 (2010); Allen, D., et al.: Eur. J. Clin. Pharmacol., 45, 313 (1993); Beer, B., et al.: J. Clin. Pharmacol., 34, 335 (1994); Rosen, A.S., et al.: Biopharm. Drug Dispos., 20, 171 (1999)<br></p>

<p>Applications MDV 3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. MDV 3100 has also been shown to induce tumor cell apoptosis, and has no agonist activity. MDV 3100 is a candidate for the treatment of castration-resistant prostate cancer.<br>References Scher, H.I. et al.: Lancet, 375, 1437 (2010); Bellmunt, J. et al.: Ther. Adv. Med. Oncol., 2, 189 (2010); Ryan, C.J. et al.: J. Clin. Oncol., 29, 3651 (2011);<br></p>

<p>Applications Pyrene occurs in coal tar. Also obtained by the destructive hydrogenation of hard coal. Found in wastewater in aquatic environments, and possesses genotoxic characteristics relating to estrogenic/androgenic, antiestrogenic and antiandrogenic activity. This compound is a contaminant of emerging concern (CECs).<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 Winterstein, et al.: Z. Physiol. Chem., 230, 162 (1934), Fang, Y. et al.: Env. Toxicol. Chem., 31, 1273 (2012);<br></p>

<p>Applications Palbociclib N-Aldehyde is an intermediate in synthesizing Palbociclib N-β-D-Glucuronide Sodium Salt (P139910), a derivative of Palbociclib (P139900) which is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.<br>References Finn, R., et al.: Breast Cancer Res., 11, 5 (2009)<br></p>

<p>Applications Labelled MDV 3100. MDV 3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. MDV 3100 has also been shown to induce tumor cell apoptosis, and has no agonist activity. MDV 3100 is a candidate for the treatment of castration-resistant prostate cancer.<br>References Scher, H.I. et al.: Lancet, 375, 1437 (2010); Bellmunt, J. et al.: Ther. Adv. Med. Oncol., 2, 189 (2010); Ryan, C.J. et al.: J. Clin. Oncol., 29, 3651 (2011);<br></p>

<p>Impurity Entacapone EP Impurity A<br>Applications cis-Entacapone (Entacapone EP Impurity A) is the (Z)-Isomer of Entacapone polymorphic form B. Antiparkinsonian.<br>References Karlsson, M., et al.: J. Pharm. Biomed. Anal., 10, 593 (1992), Nissinen, E., et al.: Arch. Pharmacol., 346, 262 (1992), Wikberg, T., et al.: Eur. J. Drug Metab. Pharmacokinet., 18, 359 (1993),<br></p>

<p>Stability Hygroscopic<br>Applications 7-Methyl Memantine is an impurity of Memantine (HCl salt, M218000) which is used as an antiparkinsonian and antispasmodic.<br>References Rohde, H., et al.: Fortschr. Med., 100, 2023 (1982), Kornhuber, J., et al.: Eur. J. Pharmacol., 166, 589 (1989), Gortelmeyer, R. and Erbler, H.: Arzneimittel-Forsch., 42, 904 (1992)<br></p>

<p>Applications Cyclopropanecarboxylic Acid is used as a reagent in the synthesis of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors. Also used as a reagent in the synthesis of 2-alkyloxazoles as potent and selective PI4KIIIβ inhibitors demonstrating inhibition of HCV replication.<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 Wang, L., et al.: Bioorg. Med. Chem. Lett., 24, 3739 (2014); Keaney, E.P., et al.: Bioorg. Med. Chem. Lett., 24, 3714 (2014)<br></p>

<p>Impurity Atenolol 2-Hydroxy Impurity<br>Applications Hydroxyatenolol is a metabolite of Atenolol (A790075); a cardioselective β-adrenergic blocker, antihypertensive, antianginal, and antiarrhythmic (class II). Atenolol 2-Hydroxy Impurity<br>References Escher, B., et al.: Environ. Sci. Technol., 40, 7402 (2006); Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984)<br></p>

<p>Stability Light Sensitive, Temperature Sensitive<br>Applications It is one of the two carotenoids contained within the retina.<br>References Karrer, et al.: Helv. Chim. Acta, 13, 268 (1930), Hlubucek, et al.: J. Chem. Soc. Perkin Trans., 1, 848 (1974), Maoka, T., et al.: Comp. Biochem. Physiol., 83B, 121 (1986),<br></p>

<p>Applications Bimatoprost Acid is an impurity of the antiglaucoma agent Bimatoprost (B386820).Bimatoprost Acid is a metabolically stable analog of PGF2α (P838625) and is a potent agonist for the FP receptor.<br>References Balapure, A.K. et al.: Biochem. Pharmacol., 38, 2375 (1989); Hellberg, M.R. et al.: J. Ocular Pharmacol. Ther., 19, 97 (2003); Krishna, P.M. et al.: J. Pharm. res., 4, 2381 (2011);<br></p>

<p>Applications An impurity of labelled Salicylic Acid synthesis<br>References Kovacik, J., et al.: J. Agric. Food Chem., 57, 9848 (2009), Gao, X., et al.: Anal. Biochem., 393, 163 (2009), Rocher, F., et al.: Plant Physiol., 150, 2081 (2009),<br></p>

<p>Applications 6-Amino-1,3-dimethyluracil is used as a reagent in the synthesis of new pyrimidine and caffeine derivatives that display highly potential antitumor activity. It is also used as a starting material in the synthesis of fused pyrido-pyrimidines.<br>References Abu-Hashem, A., et al.: Lett. Drug. Des. Discov., 12, 471 (2015); Azev, Y., et al.: Mendeleev Commun., 25, 310 (2015)<br></p>

<p>Applications 1,3-Dimethyl Barbituric Acid (Urapidil Impurity 4) is a derivative of Barbituric acid (B118650). All of the barbituric acid derivatives which have been reported to have pronounced hypnotic activity are disubstituted in the 5-position.<br>References Gupta, K., et al.: Eur. J. Med. Chem., 17, 448 (1982), Weber, L., et al.: Curr. Med. Chem., 9, 2085 (2002), Skiles, J., et al.: Curr. Med. Chem., 11, 2911 (2004),<br></p>

<p>Applications It is an indolinone derivative potently blocking VEGF-, PDGF-, and FGF-receptor kinases; an indolinone as triple angiokinase inhibitors. An antitumor agent.<br>References Sun, L., et al.: J. Med. Chem., 41, 2588 (1998); Xie, H., et al.: J. Med. Chem., 50, 4898 (2007); Hilberg, F., et al.: Cancer Res., 68, 4774 (2008); Roth, G., et al.: J. Med. Chem., 58, 1053 (2015)<br></p>

<p>Applications 1,1,1-Tris(hydroxymethyl)propane is a building block often used to make polymers. 1,1,1-Tris(hydroxymethyl)propane has been used as a precursor to prepatre alkyd resins for linseed oil based paint.<br>References Wang, X., et. al.: J. Polym. Res., 18, 721 (2011); Isiri-Caglar, D., et. al.: Rog. Org. Coat., 77, 81 (2014); Heiskanen,N., et. al.: J. Appl. Polym. Sci., 119, 209 (2011)<br></p>

<p>Applications Antitumor agent. A potent inhibitor of dihydropyrimidine dehydrogenase (DPD).<br>References Shirasaka, T., et al.: Cancer Res., 56, 2602 (1996), Patt, Y., et al.: J. Clin. Oncol., 22, 271 (2004), Shirao, K., et al.: Cancer, 100, 2355 (2004), Kelly, H., et al.: J. Clin. Oncol., 23, 4553 (2005),<br></p>

<p>Applications Simethicone is an oral anti-foaming agent used to reduce bloating, discomfort and pain caused by excess gas in the stomach or intestinal tract. Simethicone is a mixture of polydimethylsiloxane and hydrated silica gel.<br>References Grinshpan, D., et al.: Pharmaceut. Chem. J., 42, 400 (2008), Agarwal, D., et al.: J. Pharmac., 20, 206 (1988),<br></p>

<p>Impurity Atenolol EP Impurity E<br>Applications 4,4'-[(2-Hydroxy-1,3-propanediyl)bis(oxy)]bis-benzeneacetamide is an impurity of Atenolol (A790075), a cardioselective β-adrenergic blocker. Atenolol EP Impurity E<br>References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984);<br></p>

<p>Applications N-Formyl Memantine is an impurity of Memantine (M218000). Memantine impurity E per USP.<br>References Gerzon, K., et al.: J. Med. Chem., 6, 760 (1963),<br></p>

<p>Applications (E)-Isomer of labelled Entacapone polymorphic form A. Peripherally acting inhibitor of catechol-O-methyl transferase (COMT), an enzyme involved in the metabolism of catecholamine neurotransmitters and related drugs. Antiparkinsonian.<br>References Karlsson, M., et al.: J. Pharm. Biomed. Anal., 10, 593 (1992), Nissinen, E., et al.: Arch. Pharmacol., 346, 262 (1992), Wikberg, T., et al.: Eur. J. Drug Metab. Pharmacokinet., 18, 359 (1993),<br></p>

<p>Applications 5,6-Dimethylbenzimidazole (cas# 582-60-5) is a useful research chemical.<br></p>

<p>Applications N-Nitrosoatenolol is an N-nitroso derivative of Atenolol (A790075), which is a cardioselective β-adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic (class II). N-Nitrosoatenolol can be used for its genotoxic effect in rat and human hepatocytes.<br>References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984); Robbiano, L., et.al., Cancer Res., 51, 2273-2279, (1991);<br></p>

<p>Applications A potent, selective and orally active cysteinyl leukotriene type 1 receptor antagonist. Used as an antiasthmatic.<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 Matassa, V.G., et al.: J. Med. Chem., 33, 1781 (1990), Findlay, S.R., et al.: J. Allergy Clin. Immunol., 89, 1040 (1992), Krell, R.D., et al.: Am. Rev. Respir. Dis., 141, 978 (1990), Dunn, C.J., Drugs, 61, 285 (2001),<br></p>

<p>Impurity Memantine USP Related Compound B (3,5-Dimethyladamantane-1-ol)<br>Applications 3,5-Dimethyl-1-adamantanol is an impurity of Memantine (M218000). Memantine impurity B. Memantine USP Related Compound B (3,5-Dimethyladamantane-1-ol).<br>References England, P., et al.: Biochemistry, 43, 11623 (2004), Schousboe, A., et al.: Eur. J. Pharmacol., 500, 281 (2004), Horvat, S., et al.: J. Med. Chem., 49, 3136 (2006),<br></p>

<p>Applications Gentisuric Acid is a metabolite that was found in hen plasma, tissues, and eggs as a result of the consumption of naturally occurring salicylates.<br>References Protasiuk, E., &amp; Olejnik, M.: Food Addit. Contam. Part A, 37, 946 (2020)<br></p>

<p>Applications Carfilzomib is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.<br>References Fostier, K., et al.: Oncotargets. Therap., 5, 237 (2012); Geurink, P.P., et al.: J. Med. Chem., 56, 1262 (2013); McCormack, P.L., et al.: Drugs., 72, 2023 (2012);<br></p>

<p>Applications Labelled (S)-Atenolol (A790080). Cardioselective β-adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic (class II).<br>References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984),<br></p>

<p>Applications Desmethyl Nintedanib is an impurity of Intedanib (I666650), which is an antitumor agent. Desmethyl Nintedanib was used in the study of synthesizing indolinones as triple angiokinase inhibitors.<br>References Roth, G., et al.: J. Med. Chem., 52, 4466 (2009);<br></p>

<p>Applications Cardioselective β-adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic (class II).<br>References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984),<br></p>

<p>Applications Carfilzomib (2R,4S)-Diol is a derivative of Carflizomib (C183460), a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.<br>References Fostier, K., et al.: Oncotargets. Therap., 5, 237 (2012); Geurink, P.P., et al.: J. Med. Chem., 56, 1262 (2013); McCormack, P.L., et al.: Drugs., 72, 2023 (2012);<br></p>

<p>Applications 1-Hydroxypyrene-d9 is found in humane urine after exposure to coal tar and a coal derived product.<br>References Jongeneelen, F.J., et al.: Int. Arch. Occup. Environ. Health, 57, 47 (1985)<br></p>

<p>Impurity Atenolol Impurity 3; Atenolol Impurity 1<br>Applications Atenolol Impurity 3. Atenolol Impurity 1.<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 Furfural is a compound mainly found in agricultural byproducts, and is produced from the hydrolysis and dehydration of xylan contained in lignocellulose using solid acid catalysts. Furfural is also a potential platform for biofuels and inhibits fermentation in yeast.<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 Lange, J., et al.: ChemSusChem, 5, 150 (2012); Mamman, A., et al.: Biofuels, Bioprod. Biorefin., 2, 438 (2008); Navarro, A.: Curr. Microbiol., 29, 87 (1994)<br></p>

<p>Applications 3-[4-(2-methoxyphenyl)piperazin-1-yl]propan-1-amine (cas# 20529-23-1) is a useful research chemical.<br></p>

<p>Applications Carfilzomib (2R,4R)-Diol is a derivative of Carflizomib (C183460), a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.<br>References Fostier, K., et al.: Oncotargets. Therap., 5, 237 (2012); Geurink, P.P., et al.: J. Med. Chem., 56, 1262 (2013); McCormack, P.L., et al.: Drugs., 72, 2023 (2012);<br></p>

<p>Applications Azure B is a dye used for staining semi-thin sections of plant tissues. Azure B is used for staining semi-thin sections of plant tissue. This dye is also useful in the NCCLS method for blood smears and Lillie's modified Nocht's method for paraffin sections. Dyes and metabolites.<br>References 1. Penney, D.P., et al. 2002. Biotech. Histochem. 77: 237-275. PMID: 12564600<br></p>

<p>Applications Hexamethylcyclotrisiloxane is used in the preparation of Silicone coated Celgard-2400 for the adhesion of canine platelets and leucocytes.<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 Chawla, A.S.: Biomaterials, 2, 83 (1981)<br></p>

<p>Applications 7-Ketoabiraterone Acetate is an impurity of Abiraterone (A108490), a steroidal cytochrome P 450 17α-hydroxylase-17,20-lyase inhibitor (CYP17), is currently undergoing phase II clinical trials as a potential drug for the treatment of androgen-dependent prostate cancer.<br>References Denis, L., et al.: Cancer, 72, 3888 (1993); Potter, G.A., et al.: J. Med. Chem., 38, 2463 (1995); Denmeade, S., et al.: Nat. Rev., 2, 389(2002); Scher, H., et al.: J. Clin. Oncol., 23, 8253 (2005)<br></p>

<p>Applications Fulvestrant (F862500) impurity F.<br></p>

<p>Applications A metabolite of Furazolidone and Nitrofuran.Environmental contaminants; Food contaminants; Heat processing contaminants<br>References Mir, G., et al.: Indian J. Anim. Sci., 54, 888 (1984), Gottschall, D., et al.: J. Agric. Food Chem., 43, 2520 (1995)<br></p>

<p>Applications As a dye for wool and silks; as colorant in food, drugs, and cosmetics. In biochemistry as an adsorption-elution indicator for chloride estimations. Tartrazine (otherwise known as E number E102, C.I. 19140, or FD&amp;C Yellow 5) is a synthetic lemon yellow azo dye used as a food coloring. Tartrazine appears to cause the most allergic and intolerance reactions of all the azo dyes, particularly among asthmatics and those with an aspirin intolerance. Dyes and metabolites, Environmental Testing.A recent report has shown that Tartrazine may be useful in 3D bio-printing of organ-like architectures.<br>References Rowe, K.S., et al.: J. Pedriatics, 125, 691 (1994), Tanaka, T., et al.: Food Chem. Toxicol., 44, 179 (2006); Chem. and Eng News Page 4 May 6, 2019<br></p>