Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice was written by Narayanan, Sanju;Wang, Shaobin;Vasukuttan, Vineetha;Vyas Devambatla, Ravi Kumar;Dai, Donghua;Jin, Chunyang;Snyder, Rodney;Laudermilk, Lucas;Runyon, Scott P.;Maitra, Rangan. And the article was included in Journal of Medicinal Chemistry in 2021.Recommanded Product: 2-Methoxyethylamine The following contents are mentioned in the article:
Apelin receptor agonism improves symptoms of metabolic syndrome. However, endogenous apelin peptides have short half-lives, making their utility as potential drugs limited. Previously, we had identified a novel pyrazole-based agonist scaffold. Systematic modification of this scaffold was performed to produce compounds with improved ADME properties. Compound 13 (I) with favorable agonist potency (cAMPi EC50 = 162 nM), human liver microsome stability (T1/2 = 62 min), and pharmacokinetic profile in rodents was identified. The compound was tested in a mouse model of diet-induced obesity (DIO) and metabolic syndrome for efficacy. Treatment with 13 led to significant weight loss, hypophagia, improved glucose utilization, reduced liver steatosis, and improvement of disease-associated biomarkers. In conclusion, a small-mol. agonist of the apelin receptor has been identified that is suitable for in vivo investigation of the apelinergic system in DIO and perhaps other diseases where this receptor has been implicated to play a role. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Recommanded Product: 2-Methoxyethylamine).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Recommanded Product: 2-Methoxyethylamine
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem