One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, SDS of cas: 2879-20-1, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, molecular formula is C10H10O3
3-Phenylpropanoic acid-based phosphotyrosine (pTyr) mimetics: Hit evolution to a novel orally active protein tyrosine phosphatase 1B (PTP1B) inhibitor
Protein tyrosine phosphatase 1B (PTP1B) is a promising therapeutic target for type 2 diabetes. Herein, we report the evolution of a previously identified 3-phenylpropanoic acid-based PTP1B inhibitor to an orally active lead compound. A series of 3-phenylpropanoic acid-based PTP1B inhibitors were synthesized, and three of them, 3-(4-(9H-carbazol-9-yl)phenyl)-5-(3,5-di-tert-butyl-4- methoxyphenyl)-5-oxopentanoic acid (9), 3-(4-(9H-carbazol-9-yl)phenyl)-5- (4?-bromo-[1,1?-biphenyl]-4-yl)-5-oxopentanoic acid (10) and 3-(4-(9H-carbazol-9-yl)-2-fluorophenyl)-5-(4-cyclohexylphenyl)-5-oxopentanoic acid (16), showed IC50 values at sub-micromolar level. Further in vivo evaluation indicated the sodium salt of 9 not only exhibited significant insulin-sensitizing and hypoglycemia effects, but also decreased the serum levels of triglyceride and total cholesterol in high-fat-diet-induced insulin resistance model mice. Preliminary in vivo pharmacokinetic studies on the sodium salt of 9 revealed its pharmacokinetic profile after oral administration in rats. These results provide proof-of-concept for the dual effects of PTP1B inhibitors on both glucose and lipid metabolisms. A sincere form of flattery: A novel protein tyrosine phosphatase 1B (PTP1B) inhibitor with a 3-phenylpropanoic acid moiety as a phosphotyrosine (pTyr) mimetic was optimized to provide an orally active lead compound with an IC50 value of 0.40 muM against PTP1B and more notably that displayed significant in vivo activity in a murine insulin resistance model.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. SDS of cas: 2879-20-1, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 2879-20-1, in my other articles.
Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem