Add time:08/08/2019         Source:sciencedirect.com

The absorption and pharmacokinetics of Sulofenur (cas 110311-27-8) [N-(in- dan-5-sulfonyl)-N-(4-chlorophenyl)urea, LY186641] and its major metabolites were examined in mice, rats, monkeys, and dogs. The compound is a diarylsulfonylurea currently being evaluated as an oncolytic agent in phase I and II trials. In all species, sulofenur was well absorbed after an oral dose, but over a prolonged period, and sulofenur exhibited a fairly long half-life of elimination from plasma. These values ranged from 6 h in rats up to 30,110, and 200 h in mice, monkeys, and dogs, respectively, at doses (240-1000 mg/m2) within the range of those used in clinical trials. Experiments describing the high degree of binding of sulofenur to plasma proteins (consistently >99%) help to explain these relatively long half-lives. There is, however, a large difference between these plasma half-lives in the species studied. Sulofenur was previously found to be extensively metabolized to products that are excreted primarily Into the urine. In this study, its major metabolites, which are found mainly in the urine, were also minor components of the drug- related material (< 10% of the sulofenur concentrations) in the plasma of rats treated with sulofenur. The absorption, binding characteristics, and elimination of these major metabolites after their administration to rats were also compared with sulofenur. Comparison of the pharmacokinetics of sulofenur with those of other well-studied sulfonylureas of similar structure, which are metabolized in the same manner (most notably tolbutamide), suggests that for sulofenur as well, the great species difference in Its plasma half-lives may be due to differences in the rate of its oxidation to major metabolites.

We also recommend Trading Suppliers and Manufacturers of Sulofenur (cas 110311-27-8). Pls Click Website Link as below: cas 110311-27-8 suppliers