26129-32-8Relevant articles and documents
Functional and Structural Insights into Human PPARα/δ/Subtype Selectivity of Bezafibrate, Fenofibric Acid, and Pemafibrate
Akahane, Makoto,Habu, Yuki,Honda, Akihiro,Ishii, Isao,Kamata, Shotaro,Kaneko, Chihiro,Machida, Yui,Miyawaki, Saeka,Oyama, Takuji,Shiiyama, Yui,Uchii, Kie
, (2022/04/28)
Among the agonists against three peroxisome proliferator-activated receptor (PPAR) subtypes, those against PPARα (fibrates) and PPARγ (glitazones) are currently used to treat dyslipidemia and type 2 diabetes, respectively, whereas PPARδ agonists are expected to be the next-generation metabolic disease drug. In addition, some dual/pan PPAR agonists are currently being investigated via clinical trials as one of the first curative drugs against nonalcoholic fatty liver disease (NAFLD). Because PPARα/δ/γ share considerable amino acid identity and three-dimensional structures, especially in ligand-binding domains (LBDs), clinically approved fibrates, such as bezafibrate, fenofibric acid, and pemafibrate, could also act on PPARδ/γ when used as anti-NAFLD drugs. Therefore, this study examined their PPARα/δ/γ selectivity using three independent assays—a dual luciferase-based GAL4 transactivation assay for COS-7 cells, time-resolved fluorescence resonance energy transfer-based coactivator recruitment assay, and circular dichroism spectroscopy-based thermostability assay. Although the efficacy and efficiency highly varied between agonists, assay types, and PPAR subtypes, the three fibrates, except fenofibric acid that did not affect PPARδ-mediated transactivation and coactivator recruitment, activated all PPAR subtypes in those assays. Furthermore, we aimed to obtain cocrystal structures of PPARδ/γ-LBD and the three fibrates via X-ray diffraction and versatile crystallization methods, which we recently used to obtain 34 structures of PPARα-LBD cocrystallized with 17 ligands, including the fibrates. We herein reveal five novel high-resolution structures of PPARδ/γ–bezafibrate, PPARγ–fenofibric acid, and PPARδ/γ–pemafibrate, thereby providing the molecular basis for their application beyond dyslipidemia treatment.
Double emulsion techniques for making novel compositions containing gluten and polysaccharides that contain uronic acid residues useful for encapsulating fats, oils and solids
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, (2008/06/13)
Method of making compositions comprising gluten and polysaccharides that contain uronic acid residues encapsulating fats, oils and solids comprising double emulsion techniques.
Compositions containing gluten and polysaccharides that contain uronic acid residues useful for encapsulating fats, oils and solids
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, (2008/06/13)
The present invention relates to compositions useful for encapsulating fats, oils or solids, comprising gluten and polysaccharides that contains uronic acid residues.
Pesticidal concentrate compositions
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, (2008/06/13)
A pesticidal concentrate comprising a pesticidal component suspended in an oily component, the composition comprising 1-55% by weight of pesticide, 20-90% by weight of the oily component and 1-45% by weight of a surfactant component, and optionally water and optionally filler, the surfactant component comprising one or more stabilizing constituents comprising a C5-30 hydrocarbylene chain carrying a group capable of forming hydrogen bonds with water, and optionally one or more other constituents selected from the group consisting of non-ionic and ionic surfactants, the stabilizing constituent being present in an amount of at least 4% by weight, calculated on the total amount of surfactant component in the composition. Examples of stabilizing constituents are fatty alcohols and amino group-containing surfactants, especially ampholytes. Pesticidal concentrate compositions comprising 1-55% by weight of finely ground dithiocarbamate or glyphosate suspended in 10-90% by weight of an oily component and comprising 1-50% by weight of a surfactant component, calculated on the total composition, may be prepared. The pesticidal concentrate compositions are used in the preparation of ready-to-use-spray liquid, normally comprising 0.1-10% of concentrate and 90-99.9% of water.
Herbicidal esters of D-1-(phenoxy-4-phenoxy)propionic acid
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, (2008/06/13)
Optically active enantiomers of the formula I STR1 where R is a group of the formulae STR2 R1 and R2, among others, are halogen or CF3 and Z is a carboxyl, carboxylate, carboxylic acid ester, thioester, carbonamide, carboxylic acid anilide, carbohydrazide or thioamide group, are interesting herbicides the effect of which is considerably superior to that of the optically inactive racemates.
Process for the preparation of (phenoxy- or benzyl-)-phenoxypropionic acids and their alkali metal salts
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, (2008/06/13)
Process for the preparation of (phenoxy- or benzyl-)-phenoxypropionic acids and the alkali metal salts thereof by adding a double molar amount of an aqueous alkali hydroxide to a boiling mixture of a (benzyl- or phenoxy-)-phenol and 2-chloropropionic acid
2-[P-(p-Substituted phenoxy)phenoxy]propionyl oximes
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, (2008/06/13)
2-[p-(p-substituted phenoxy)phenoxy] propionyl oximes, processes for their preparation, herbicidal compositions containing these oximes and methods of use of the herbicidal compositions are disclosed.
HCG 004, a new highly potent hypolipidaemic drug
Granzer,Nahm
, p. 1353 - 1354 (2007/10/06)
In normolipidemic and hyperlipidemic animals 2 [4(4' chlorophenoxy) phenoxy] propionic acid (HCG 004) is a well tolerated and highly effective oral hypolipidemic drug. Within the hypolipidemically interesting dosage range no other pharmacological or chronic toxicological effects were found contraindicating the therapeutic use in humans.