FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2023160592> ?p ?o ?g. }

• W2023160592 endingPage "125" @default.
• W2023160592 startingPage "119" @default.
• W2023160592 abstract "Peroxisome proliferator-activated receptor (PPAR) α and γ are key regulators of lipid homeostasis and insulin resistance. In this study, we characterize the pharmacological profiles of PAR-5359, a dual agonist of PPARα and γ with well-balanced activities. In transient transactivation assay, PAR-5359 (3-(4-{2[4-(4chloro-phenyl)-3,6-dihydro-2H-pyridin-1-yl]-ethoxy}-phenyl)-(2S)-ethoxy-propionic acid) significantly activated human and mouse PPARα and γ without activating PPARδ. In functional assays using human mesenchymal stem cells and human hepatoma HepG2 cells, PAR-5359 significantly induced adipocyte differentiation and human ApoA1 secretion, which coincided with its transactivation potencies against the corresponding human receptor subtypes. Interestingly, PAR-5359 showed equivalent potencies against the mouse receptor subtypes (α and γ; 2.84 μM and 3.02 μM, respectively), which suggests the possibility that PAR-5359 could simultaneously activates each subtype of receptors subtype in under physiological conditions. In an insulin-resistant ob/ob mouse model, PAR-5359 significantly reduced plasma insulin levels, improved insulin sensitivity (HOMA-IR), and completely normalized plasma glucose levels. In a severe diabetic db/db mouse model, PAR-5359 dose-dependently reduced the plasma levels of glucose (ED30 = 0.07 mg/kg). Furthermore, it lowered plasma levels of non HDL- (ED30 = 0.13 mg/kg) and total cholesterol (ED30 = 0.03 mg/kg) in high cholesterol diet-fed rats for 4 days treatment. These results suggest that PAR-5359 has the balanced activities for PPARα and PPARγ in vivo as well as in vitro. And its balanced activities may render PAR-5359 as a pharmacological tool in elucidating the complex roles of PPARα/γ dual agonists." @default.
• W2023160592 created "2016-06-24" @default.
• W2023160592 creator A5001687474 @default.
• W2023160592 creator A5007506066 @default.
• W2023160592 creator A5008159288 @default.
• W2023160592 creator A5021970093 @default.
• W2023160592 creator A5023335726 @default.
• W2023160592 creator A5025023052 @default.
• W2023160592 creator A5028671401 @default.
• W2023160592 creator A5036707986 @default.
• W2023160592 creator A5036880791 @default.
• W2023160592 creator A5037008723 @default.
• W2023160592 creator A5048043371 @default.
• W2023160592 creator A5064605421 @default.
• W2023160592 creator A5070894169 @default.
• W2023160592 creator A5085184229 @default.
• W2023160592 creator A5089777700 @default.
• W2023160592 creator A5090316763 @default.
• W2023160592 date "2008-10-01" @default.
• W2023160592 modified "2023-10-16" @default.
• W2023160592 title "PAR-5359, a well-balanced PPARα/γ dual agonist, exhibits equivalent antidiabetic and hypolipidemic activities in vitro and in vivo" @default.
• W2023160592 cites W1964448491 @default.
• W2023160592 cites W1965907725 @default.
• W2023160592 cites W1974569331 @default.
• W2023160592 cites W1977004017 @default.
• W2023160592 cites W2017029824 @default.
• W2023160592 cites W2021435938 @default.
• W2023160592 cites W2022684565 @default.
• W2023160592 cites W2032245476 @default.
• W2023160592 cites W2034567556 @default.
• W2023160592 cites W2047982128 @default.
• W2023160592 cites W2049702067 @default.
• W2023160592 cites W2055503413 @default.
• W2023160592 cites W2055726721 @default.
• W2023160592 cites W2055943486 @default.
• W2023160592 cites W2056939999 @default.
• W2023160592 cites W2062551263 @default.
• W2023160592 cites W2073801053 @default.
• W2023160592 cites W2074413591 @default.
• W2023160592 cites W2075284190 @default.
• W2023160592 cites W2087718039 @default.
• W2023160592 cites W2092621119 @default.
• W2023160592 cites W2093104742 @default.
• W2023160592 cites W2094229974 @default.
• W2023160592 cites W2102906564 @default.
• W2023160592 cites W2107298817 @default.
• W2023160592 cites W2112869240 @default.
• W2023160592 cites W2113347778 @default.
• W2023160592 cites W2127307547 @default.
• W2023160592 cites W2127456444 @default.
• W2023160592 cites W2139315494 @default.
• W2023160592 cites W2146363516 @default.
• W2023160592 cites W2159270178 @default.
• W2023160592 cites W2164015929 @default.
• W2023160592 cites W2318286563 @default.
• W2023160592 cites W36311596 @default.
• W2023160592 doi "https://doi.org/10.1016/j.ejphar.2008.07.066" @default.
• W2023160592 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18727927" @default.
• W2023160592 hasPublicationYear "2008" @default.
• W2023160592 type Work @default.
• W2023160592 sameAs 2023160592 @default.
• W2023160592 citedByCount "29" @default.
• W2023160592 countsByYear W20231605922012 @default.
• W2023160592 countsByYear W20231605922013 @default.
• W2023160592 countsByYear W20231605922015 @default.
• W2023160592 countsByYear W20231605922017 @default.
• W2023160592 countsByYear W20231605922021 @default.
• W2023160592 countsByYear W20231605922022 @default.
• W2023160592 countsByYear W20231605922023 @default.
• W2023160592 crossrefType "journal-article" @default.
• W2023160592 hasAuthorship W2023160592A5001687474 @default.
• W2023160592 hasAuthorship W2023160592A5007506066 @default.
• W2023160592 hasAuthorship W2023160592A5008159288 @default.
• W2023160592 hasAuthorship W2023160592A5021970093 @default.
• W2023160592 hasAuthorship W2023160592A5023335726 @default.
• W2023160592 hasAuthorship W2023160592A5025023052 @default.
• W2023160592 hasAuthorship W2023160592A5028671401 @default.
• W2023160592 hasAuthorship W2023160592A5036707986 @default.
• W2023160592 hasAuthorship W2023160592A5036880791 @default.
• W2023160592 hasAuthorship W2023160592A5037008723 @default.
• W2023160592 hasAuthorship W2023160592A5048043371 @default.
• W2023160592 hasAuthorship W2023160592A5064605421 @default.
• W2023160592 hasAuthorship W2023160592A5070894169 @default.
• W2023160592 hasAuthorship W2023160592A5085184229 @default.
• W2023160592 hasAuthorship W2023160592A5089777700 @default.
• W2023160592 hasAuthorship W2023160592A5090316763 @default.
• W2023160592 hasConcept C104317684 @default.
• W2023160592 hasConcept C126322002 @default.
• W2023160592 hasConcept C1292079 @default.
• W2023160592 hasConcept C134018914 @default.
• W2023160592 hasConcept C150903083 @default.
• W2023160592 hasConcept C170493617 @default.
• W2023160592 hasConcept C185592680 @default.
• W2023160592 hasConcept C187345961 @default.
• W2023160592 hasConcept C202751555 @default.
• W2023160592 hasConcept C207001950 @default.
• W2023160592 hasConcept C2777391703 @default.
• W2023160592 hasConcept C2778938600 @default.

• next