Enzimi inibitori

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 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 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)

Applications 4-Hydroxypiperidine-D4 is an isotope labelled form of 4-Hydroxypiperidine (H950845), a reagent for the synthesis of acridine (A190900) derivatives and fibrinogen receptor antagonists.
References Yang, D. et al.: Macromol., 35, 5304 (2002); Harrison, R.J. et al.: Bioorg. Med. Chem. Lett., 9, 2463 (1999);

Applications Valtrate is a Rev-transport inhibitor with anti-HIV activity from Valerianae Radix.
References Murakami, N., et al.: Bioorg. Med. Chem. Lett., 12, 2807 (2002); Watanabe, K., et al.: Drug Discoveries Ther., 5, 26 92011)

Stability Hygroscopic
Applications (3R,5S,6E)-7-(2-cyclopropyl-4-phenyl-3-quinolinyl)-3,5-dihydroxy-6-heptenoic Acid Sodium Salt is an impurity of Pitavastatin (P531000), a HMG CoA reductase inhibitor and an antilipemic agent.
References Suzukim M., et al.: Bioorg. Med. Chem., 9, 2977 (1999); Yen, H., et al.: J. Clin. Invest., 98, 1253 (1996); Zou, Y., et al.: J. Biol. Chem., 274, 9760 (1999); Sun, X., et al.: Cancer Res., et al.: 61, 3382 (2001); Ladas, E.J., et al.: Clin. Oncol., 22, 517 (2004);

Stability Hygroscopic
Applications Labelled (-)-Epigallocatechin Gallate, a tumor-inhibiting constituent of green tea. (-)-Epigallocatechin Gallate alters the cleavage of amyloid precursor protein, decreasing production of amaloid-ß and amaloid plaques in mice.
References Yamane, T. et al.: Cancer Res., 55, 2081 (1995); Tan, J. et al.: J. Neurosci. 25, 8807 (2005);

Applications K252a is a protein kinase inhibitor. It is an analogue of staurosporine (S685000). It shows potent antitumor activity but no antimicrobial activity in vitro, or in vivo toxicity in rodents.
References Kase, H., et al.: J. Antibiot., 39, 1059 (1986); Yasuzawa, T., et al.; J. Antibiot., 39, 1072 (1986)

Stability Hygroscopic
Applications An extremely potent and selective a-D-mannosidase inhibitor.

Applications Labelled 2-(3,4-Dimethoxyphenyl)-N-methylethylamine (D470710, free amine) which is a methylated metabolite of Dopamine (D533780); a potent inhibitor of brain mitochondrial respiration used in Parkinson’s disease studies.
References Gluck, M.R. et al.: J. Neurochem., 91, 788 (2004); Charlton, C.G. et al.: Life Sci., 66, 2159 (2000);

Applications rac-syn-Ezetimibe is an analog of Ezetimibe (E975000); an antihyperlipoproteinemic and a cholesterol absorption inhibitor.
References van Heek, M., at al.: J. Pharmacol. Exp. Ther., 283, 157 (1997); van Heek, M., at al.: Brit. J. Pharmacol., 129, 1748 (2000)