Inhibiteur d’enzymes

Stability Moisture, Temperature Sensitive; Hygroscopic
Applications A putative lipid second messenger; found to inhibit cellular mobility of melanoma cells at very low concentrations with no toxic effects thereby making it a possible agent for prevention of tumor cell metastasis and inflammatory processes. It mobilizes intracellular calcium stores, decreases cellular cAMP, activates phospholipase D and does not inhibitprotein kinase C.
References Yeh, C., et al.: Am. J. Physiol., 296, H1193 (2009), Hagen, N., et al.: J. Biol. Chem., 284, 11346 (2009), Kuehnel, M., et al.: J. Cell Sci., 122, 499 (2009),

Applications (3S,4S,3’S)-Ezetimbe is a 3-epimer impurity of Ezetimibe (E975000), 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)

Applications 2-(Hydroxyamino)acetic Acid is a novel lactase inhibitor.
References Hattori, M., et al.: J. Insect Physiol., 51, 1359 (2005); Murao, S., et al.: Biosci. Biotech. Biochem., 56, 987 (1992)

Stability Hygroscopic
Applications A glucosidase inhibitor.
References Fellows, L.E.: Pestic. Sci., 17, 602 (1986)

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),

Impurity Atorvastatin Related Compound E
Applications Impuritiy of Atorvaststin (A791750), a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia. Atorvastatin Related Compound E
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993), Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996), Whitfield, L.R., et al.: Eur. J. Drug Metab. Pharmacokinet., 25, 97 (2000),

Applications Teneligliptin Hydrobromide (2:5) is a dipeptidyl peptidase-4 (DPP-4) inhibitor that is used to treat type 2 diabetes. It is eliminated via excretion, and has a half-life of 24.2 hours in the human body.
References Goda, M. & Kadowaki, T.: Drugs Today, 49, 615 (2013); Kishimoto, M.: Diabetes Metab. Syndr. Obes., 6, 187 (2012)

Applications N-Alkyl phosphoric triamide useful as urease inhibitors.

Stability Hygroscopic
Applications α-Glycosidase inhibitor.
References van de Water, F., et al.: Drug Metab. Rev., 37, 443 (2005), Koepsell, H., et al.: Pharm. Res., 24, 1227 (2007), Jappar, D., et al.: Pharm. Res., 26, 172 (2009),

Applications Nitromifene citrate is a non-steroidal estrogen antagonist. It is structurally similar to Tamoxifen (T006000) which is a selective estrogen response modifier (SERM).
References Rudick, C., et al.: Endorcrinol., 144, 179 (2003); Sutherland, R., et al.: Nature, 267, 434 (1977)

Stability Hygroscopic
Applications Vitamin B12 Monocarboxylic Acid is an impurity of Vitamin B12 (V676005) which is a water-soluble vitamin with a key role in the normal functioning of the brain and nervous system, and for the formation of blood.
References Rickes, et al.: Science, 107, 396 (1948); Kirschbaum, J., et al.: Anal. Profiles Drug Subs., 10, 183 (1981); Grasbeck, R., et al.: Clin. Biochem., 17, 99 (1984)

Applications An inhibitor of phosphodiesterase IV, about 8 times more active for cAMP than cGMP.
References Chesin, et al.: Biochem. Pharmacol., 21, 2443 (1972), Ahluwalia, et al.: Biochem. Pharmacol., 31, 665 (1982), Nicholson, et al.: TIPS, 12, 19 (1991),