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Usage

Uses

Used in Pharmaceutical Industry:
LT175 is used as a dual PPARα/γ ligand for its potential therapeutic effects on glucose homeostasis and insulin resistance. Its low adipogenic activity in vitro makes it a promising candidate for the development of treatments targeting metabolic disorders and related conditions.

Biological Activity

lt175 is a dual pparα/γ ligand.peroxisome proliferator-activated receptors (ppars) are ligand-dependent transcription factors regulating lipid and glucose metabolism.

in vitro

lt175 was identified as a partial agonist against pparγ and interacted with a newly identified region of the pparγ-ligand binding domain. lt175 could differentially activate pparγ target genes involved in fatty acid esterification and storage, resulting in a less severe lipid accumulation compared with that triggered by rosiglitazone. moreover, the peculiar interaction of lt175 with pparγ could affect the recruitment of the coregulators cyclic-amp response element-binding protein-binding protein and nuclear corepressor 1 [1].

in vivo

animal in vivo study showed that the administration of lt175 to mice fed a high-fat diet could decrease the adipocyte size, body weight, as well as white adipose tissue mass, as measured by magnetic resonance imaging. in addition, lt175 was able to significantly reduce the insulin, plasma glucose, triglycerides, non-esterified fatty acids, and cholesterol and also could increase the levels of circulating adiponectin and fibroblast growth factor 21. moreover, the oral glucose and insulin tolerance tests showed that lt175 could improve glucose homeostasis and insulin sensitivity [1].

references

[1] gilardi f et al. lt175 is a novel pparα/γ ligand with potent insulin-sensitizing effects and reduced adipogenic properties. j biol chem. 2014 mar 7;289(10):6908-20.

Upstream product

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Relevant academic research and scientific papers

Preparation method of para-substituted aryl compound

The invention discloses a preparation method of a para-substituted aryl compound shown as a formula (I) which is described in the specfication. The preparation method is characterized by comprising the following step of: subjecting an aryl sulfonium salt shown as a formula (II) which is described in the specfication and boride to a coupling reaction in a solvent in an inert atmosphere under the action of alkali and a palladium catalyst to obtain the para-substituted aryl compound. According to the method, mono-substituted aromatic hydrocarbon is taken as a substrate, the aryl sulfonium salt isconstructed in situ, and the palladium catalyst catalyzes the aryl sulfonium salt constructed in situ to undergo the Suzuki-Miyaura coupling reaction, so a mono-substituted aromatic hydrocarbon para-arylation or alkenylation product is constructed quickly and efficiently. The method is mild in conditions, high in substrate universality and wide in tolerance of a heterocyclic coupling substrate.

para-Selective arylation and alkenylation of monosubstituted arenes using thianthreneS-oxide as a transient mediator

Using thianthreneS-oxide (TTSO) as a transient mediator,para-arylation and alkenylation of mono-substituted arenes have been demonstratedviaapara-selective thianthrenation/Pd-catalyzed thio-Suzuki-Miyaura coupling sequence under mild conditions. This reaction features a broad substrate scope, and functional group and heterocycle tolerance. The versatility of this approach was further demonstrated by late-stage functionalization of complex bioactive scaffolds, and direct synthesis of some pharmaceuticals, including Tetriprofen, Ibuprofen, Bifonazole, and LJ570.

Crystal structure of the peroxisome proliferator-activated receptor γ (PPARγ) ligand binding domain complexed with a novel partial agonist: A new region of the hydrophobic pocket could be exploited for drug design

The peroxisome proliferator-activated receptors (PPARs) are ligand-dependent transcription factors regulating glucose and lipid metabolism. The search for new PPAR ligands with reduced adverse effects with respect to the marketed antidiabetic agents thiaz

Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARα and PPARγ agonist activity

Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors that govern lipid and glucose homeostasis playing a central role in cardiovascular diseases, obesity, and diabetes. Medications targeted to PPARs have been esta