Inhibitor Enzymes

Stability Hygroscopic
Applications Raloxifene 4’-Glucuronide Lithium Salt is a metabolite of Raloxifene (R099995), a nonsteroidal estrogen receptor mixed agonist/antagonist.
References Dodge, J., et al.: Bioorg. Med. Chem. Lett., 7, 993 (1997); Jeong, E., et al.: Drug Metab. Dispos., 33, 785 (2005); Trontelj, J., et al.: Pharmacol. Res., 52, 334 (2005); Oswald, S., et al.: Clin. Pharmacol. Ther., 79 206 (2006)

Stability Hygroscopic
Applications α-Glycosidase inhibitor.
References Jefferies, I., et al.: Bioorg. Med. Chem. Lett., 7, 1171 (1997), Hassan, A., et al.: Carbohydr. Res., 339, 1565 (2004),

Stability Air and Moisture Sensitive
Applications N-[4-Amino-2-chloro-6-[(2-deoxy-2-fluoro-α-D-arabinopyranosyl)amino]-5-pyrimidinyl]-formamide is a clofarabine related compound. Clofarabine (C586890) is a second generation purine nucleoside analog; antimetabolite that inhibits DNA synthesis and resists deamination by adenosine deaminase. Antineoplastic.
References Gandhi, V., et al.: Clin. Cancer Res., 9, 6335 (2003), Kantarjian, H., et al.: Blood, 102, 2379 (2003), Faderl, S., et al.: Cancer, 103, 1985 (2005),

Applications 4-Fluorobenzoic Acid-d4 is used as a reagent in the synthesis of Flurofamide-d4 (F596687); the isotope labelled analog of Fluorofamide (F596685) which is a compound that acts as a urease inhibitor, useful in the treatment of gastritis and irregular urease activity in the urinary tract.
References Loes, A. et al.: Lett. App. Microbiol., 58, 31 (2014); Ohta, T.et al.: Biochem. Biophys, Res. Comm., 285, 728 (2001)

Applications n-Pentyl-d11 chloroformate is labelled n-Pentyl chloroformate which can be used to synthesize 1,3-disubstituted ureas as potent inhibitors of the soluble epoxide hydrolase.
References Kim, I., et al.: J. Med. Chem., 47, 2110 (2004); Hammock, B., et al.: PCT Int. Appl. (2006), WO 2006045119 A2 20060427.

Applications 4-​Pyridin-​2,​3,​5,​6-​d4-​ol-​d is one of the azepanone derivatives studies as CGRP receptor antagonists.
References Liu, J.: PCT Int. Appl. (2010), WO 2010108103 A1 20100923.

Applications Isotope labelled O-Desethyl Azilsartan is an active metabolite of TAK-491 which acts as a new angiotensin II receptor antagonist.
References Kawaguchi, N. et al.: Xenobiotica, 43, 182 (2013);

Applications n-Propyl-2,2,3,3,3-d5-amine Hydrochloride is the hydrochloride salt of 1-Propyl-d5-amine (P833702); the isotope labelled analog of 1-Propylamine (P833700) which is used in the synthesis of pyrimidine derivatives as novel and highly potent PDE4 inhibitors. It is also used in the preparation of fluorenone analogs with DNA topisomerase I inhibitors.
References Goto, T. et al.: Bioorg. Med. Chem., 21, 7025 (2013); Lee, C. et al.: Bioorg. Med. Chem. 21, 7125, (2013)

Applications JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor.
References Hatcher, J.M.; et al.: ACS Med. Chem. Lett., 6, 584 (2015)

Applications A labelled fatty acid found in Amaranth oil; it shows inhibitory activity.
References Fidler, N., et al.: J. Lipid Res., 41, 1376 (2000), Yang, T., et al.: Food Chem., 80, 473 (2003), Gamel, T., et al.: J. Food Lipids, 14, 323 (2007),

Applications A metabolite of the chemotherapeutic drug Tamoxifen (T006000). Exhibits a more potent estrogen agonist/antagonist activity than the parent drug. Also active as an intramembranous inhibitor of lipid peroxidation.
References Kupfer, D., et al.: Cancer Res., 54, 3140 (1994), Custodio, J.B.A., et al.: Biochem. Pharmacol., 47, 1989 (1994),

Applications Ceramide-1-phosphate blocks apoptosis through inhibition of acid sphingomyelinase in macrophages.
References Furukawa, A., et al.: Mol. Cell. Biochem., 305, 27 (2007), Chen-Quay, S., et al.: J. Pharm. Sci., 98, 606 (2009),

Applications 1-Propyl-d5-amine is labelled 1-Propylamine (P833700) which is used in the synthesis of pyrimidine derivatives as novel and highly potent PDE4 inhibitors. It is also used in the preparation of fluorenone analogs with DNA topisomerase I inhibitors.
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 B-[2-(Methylamino)-4-pyridinyl]boronic Acid Hydrochlroide, is used to prepare novel selective thiazoleacetic acids as CRTH2 antagonists.
References Grimstrup, M., et al.: Bioorg. Med. Chem. Lett., 20, 1181 (2010)