Inhibitor Enzymes

Applications A potent inhibitor of estrone sulfatase. Inhibits estrone sulfatase >99% at 0.1uM in intact MCF-7 cells, IC50=65pM.
References Woo, L.W., et al.: J. Med. Chem., 41, 1068 (1998)

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)

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

Stability Moisture and Temperature Sensitive
Applications Galacto-PUGNAc is a highly selective inhibitor for β-hexosaminidases HEXA and HEXB is cell-permeable. Galacto-PUGNAc is able to modulate the activity of HEXA and HEXB in tissue culture, increasing ganglioside GM2 levels in neuroblastoma cells
References Stubbs, K.A. et al.: Angew. Chem. Int. Ed., 48, 1300 (2009);

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 An inhibitor of fatty acid oxidation. Aminocarnitine acts as a hypoglycemic and antiketogenic compound. It alters lipidic metabolism by inhibiting carnitine acetyltransferase (CAT) and carnitine palmitoyltransferase (CPT).
References Jenkins, D.L., et al.: J. Biol. Chem., 260, 14748 (1985), Kanamaru, T., et al.: M. Life Sci., 37, 217 (1985), Hulsmann, W.C., et al.: J. Biochim. Biophys. Acta., 1097, 263 (1991), Chiodi, P., et al.: Biochim, Biophys. Acta., 1127, 81 (1992),

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)

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 N-Alkyl phosphoric triamide useful as urease inhibitors.

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 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)

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 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)