856251-39-3Relevant academic research and scientific papers
Multifunctional core-shell silica nanoparticles for highly sensitive 19F magnetic resonance imaging
Matsushita, Hisashi,Mizukami, Shin,Sugihara, Fuminori,Nakanishi, Yosuke,Yoshioka, Yoshichika,Kikuchi, Kazuya
, p. 1008 - 1011 (2014)
19F magnetic resonance imaging (19F MRI) is useful for monitoring particular signals from biological samples, cells, and target tissues, because background signals are missing in animal bodies. Therefore, highly sensitive 19/su
Addressing hERG activity while maintaining favorable potency, selectivity and pharmacokinetic properties of PPARδ modulators
Lagu, Bharat,Senaiar, Ramesh S.,Kluge, Arthur F.,Mallesh,Ramakrishna,Bhat, Raveendra,Patane, Michael A.
, (2020/01/03)
One of the most commonly used strategies to reduce hERG (human ether-a-go-go) activity in the drug candidates is introduction of a carboxylic acid group. During the optimization of PPARδ modulators, some of the compounds containing a carboxylic acid were found to inhibit the hERG channel in a patch clamp assay. By modifying the basicity of the imidazole core, potent and selective PPARδ modulators that do not inhibit hERG channel were identified. Some of the modulators have excellent pharmacokinetic profiles in mice.
PPAR AGONISTS, COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
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Page/Page column 45; 61, (2017/11/10)
Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
Novel affinity ligands for chromatography using combinatorial chemistry
Regberg, Tor,Lindquist, Charlotta,Pilotti, Ake,Ellstroem, Christel,Faegerstam, Lars,Eckersten, Ann,Shinohara, Yasuro,Gallion, Steven L.,Hogan Jr., Joseph C.
experimental part, p. 267 - 278 (2012/05/05)
Spatially addressable combinatorial libraries were synthesized by solution phase chemistry and screened for binding to human serum albumin. Members of arylidene diamide libraries were among the best hits found, having submicromolar binding affinities. The results were analyzed by the frequency with which particular substituents appeared among the most potent compounds. After immobilization of the ligands either through the oxazolone or the amine substituent, characterization by surface plasmon resonance showed that ibuprofen affected the binding kinetics, but phenylbutazone did not. It is therefore likely that these compounds bind to Site 2 in sub domain IIIA of human serum albumin (HSA).
NOVEL GLUCAGON ANTAGONISTS/INVERSE AGONISTS
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Page/Page column 25-26, (2010/02/12)
Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.
