One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, molecular formula is C7H4ClNO3
Lack of correlation between in vitro and in vivo studies on the inhibitory effects of (-)-sophoranone on CYP2C9 is attributable to low oral absorption and extensive plasma protein binding of (-)-sophoranone
(-)-Sophoranone (SPN) is a bioactive component of Sophora tonkinensis with various pharmacological activities. This study aims to evaluate its in vitro and in vivo inhibitory potential against the nine major CYP enzymes. Of the nine tested CYPs, it exerted the strongest inhibitory effect on CYP2C9-mediated tolbutamide 4-hydroxylation with the lowest IC50 (Ki) value of 0.966 ¡À 0.149 muM (0.503 ¡À 0.0383 muM), in a competitive manner. Additionally, it strongly inhibited other CYP2C9-catalyzed diclofenac 4′-hydroxylation and losartan oxidation activities. Upon 30 min preincubation of human liver microsomes with SPN in the presence of NADPH, no obvious shift in IC50 was observed, suggesting that SPN is not a time-dependent inactivator of the nine CYPs. However, oral co-administration of SPN had no significant effect on the pharmacokinetics of diclofenac and 4′-hydroxydiclofenac in rats. Overall, SPN is a potent inhibitor of CYP2C9 in vitro but not in vivo. The very low permeability of SPN in Caco-2 cells (Papp value of 0.115 ¡Á 10-6 cm/s), which suggests poor absorption in vivo, and its high degree of plasma protein binding (>99.9%) may lead to the lack of in vitro-in vivo correlation. These findings will be helpful for the safe and effective clinical use of SPN.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. name: 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 1750-45-4, in my other articles.
Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem