Chemical Biology and Drug Design
SEPTEMBER 20, 2023
Magnoflorine increased the systemic exposure and metabolic stability and suppressed the transport of luteolin. CaCO-2 cell transwell assay was employed for transport evaluation, and the metabolic stability of luteolin and CYP3A activity were assessed in rat liver microsomes.
Chemical Biology and Drug Design
JUNE 8, 2023
The co-administration of cryptotanshinone with ophiopogonin D induced pharmacokinetic interaction prolonging the systemic exposure and improving metabolic stability of cryptotanshinone. The Caco-2 cells were employed to evaluate the transport of cryptotanshinone, and the metabolic stability was studied in the rat liver microsomes.
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Chemical Biology and Drug Design
OCTOBER 5, 2023
However, the aldehyde functional group metabolic instability has severly hampered their development, except for voxelotor, which was approved in 2019 for SCD treatment.
Molecular Design
OCTOBER 20, 2024
One way of doing this is to build models for predicting biological activity and other pharmaceutically relevant properties such as aqueous solubility, permeability and metabolic stability.
Metabolite Tales Blog
JULY 5, 2023
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13]. Balazs et al.,
Metabolite Tales Blog
JULY 5, 2023
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13]. Balazs et al.,
Molecular Design
MAY 11, 2019
I'll examine an article entitled ‘Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations’ (YL2018) in this post and I should note that the article title reminded me that abseiling has been described as the second fastest way down the mountain.
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