Metabolic Effects of a New Hypolipidemic Agent, Ciprofibrate

Effects of KRN4884, a novel pyridinecarboxamidine type KATP channel opener, on serum triglyceride levels in rats

“…Because a reduction in circulating levels of free fatty acid should decrease the availability of free fatty acid to the liver to serve as a substrate for the synthesis of triglyceride (Grundy & Vega, 1987), clofibrate‐induced reduction in TGSR is likely to be related to the inhibition of hepatic triglyceride formation by clofibrate (Adams et al , 1971). The reduction in serum free fatty acid levels by clofibrate is thought to result from: decrease in free fatty acid synthesis (Maragoudakis et al , 1972; Strandberg et al , 1983); reduced mobilization of free fatty acid (Arnold et al , 1979) and increased β‐oxidation of fatty acid (Vainio et al , 1983; Alegret et al , 1994). On the other hand, while KRN4884 resulted in a TGSR reduction, it was not significant and was less extensive as compared to that induced by clofibrate treatment.…”

Discovery of a New CDK4/6 and PI3K/AKT Multiple Kinase Inhibitor Aminoquinol for the Treatment of Hepatocellular Carcinoma

“…The compounds were sorted in an ascending order according to their average predicted binding free energy, and the high-scoring compounds were manually examined based on in silico estimations of binding strength, appropriate molecular weight and other drug-like properties, complementary matching of molecular shape, plus some sense of intuition from a computational chemist's experience. Finally, high-scoring compounds were shortlisted and 10 commercially available compounds (Supplementary Table 1) (Bueno 1965;Janssen et al, 1968;Ross 1970;Arnold et al, 1979;Dejana et al, 1982;Lassus et al, 1983;Fujimaki et al, 1988;Matsumoto et al, 1994;Muscatello et al, 2014) were purchased for subsequent wet-lab validations.…”

Zur Pharmakokinetik von Lipidsenkern, 4. Mitt.: Biotransformation des Lipidsenkers Ciprofibrat (2‐(4‐(2,2‐Dichlorcyclopropyl)‐phenoxy)‐2‐methylpropionsäure)

“…Theoretisch ware die enzymatische Spaltung der Ether-Bindung in Ar-O-C(CH,),COOH auch nicht zu erklaren, da die oxidative Entalkylierung, die zuerst von MucMuhorz? postuliert worden war, strukturell davon abhangig ist, da13 dem (1). Freies Ciprofibrat tritt praktisch im Blasenharn nicht auf, bildet sich aber beim Stehen des Untersuchungsmaterials infolge der Anwesenheit von P-Glukuronidasen im Sammelharn.…”