We have discovered a novel small-molecule (3-phosphinoylpropionic acid) inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa), BX 528, which had an IC 50 of 2 nM in an enzymatic assay and 50 nM in an in-vitro clot lysis assay, with 3,500- to 35,000-fold selectivity against other carboxypeptidases, such as CPN, CPZ and CPD, and 5- and 12-fold selectivity against CPE (CPH) and CPB, respectively...
Keywords: TAFI, carboxypeptidases, potency, selectivity, safety, pharmacokinetics
01/2007 | Thrombosis and Haemostasis, SchattauerIn the presence of oxygen, radiolytically generated carbonate radical anions, CO3?–, were reacted with methyl ?-D-cellobioside and methyl ?-D-glucoside...
Keywords: carbohydrate, carbonate radical, glucosidic cleavage, hydrogen abstraction, intramolecular, model compounds, selectivity
03/2006 | Holzforschung, Walter de GruyterA series of long chain isonicotinamides (pyridine-4-carboxamides) and dipicolinamides (pyridine-2,6-dicarboxamides) have been prepared with different substituting groups and the extracting ability for Fe(III), Am(III), Eu(III), Sr(II), Co(II) and Cs(I) from nitric acid solutions has been studied...
Keywords: Extraction, Isonicotinamides, Dipicolinamides, Radiolysis, selectivity
09/2007 | Radiochimica Acta, Oldenbourg Wissenschaftsverlag