Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Their Common Age-Related Comorbidities was written by Cioffi, Christopher L.;Raja, Arun;Muthuraman, Parthasarathy;Jayaraman, Aravindan;Jayakumar, Srinivasan;Varadi, Andras;Racz, Boglarka;Petrukhin, Konstantin. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 82702-31-6 This article mentions the following:
Dissociation of transthyretin (TTR) tetramers may lead to misfolding and aggregation of proamyloidogenic monomers, which underlies TTR amyloidosis (ATTR) pathophysiol. ATTR is a progressive disease resulting from the deposition of toxic fibrils in tissues that predominantly presents clin. as amyloid cardiomyopathy and peripheral polyneuropathy. Ligands that bind to and kinetically stabilize TTR tetramers prohibit their dissociation and may prevent ATTR onset. Drawing from clin. investigated AG10, we designed a constrained congener (14) that exhibits excellent TTR tetramer binding potency, prevents TTR aggregation in a gel-based assay, and possesses desirable pharmacokinetics in mice. Addnl., 14 significantly lowers murine serum retinol binding protein 4 (RBP4) levels despite a lack of binding at that protein′s all-trans-retinol site. We hypothesize that kinetic stabilization of TTR tetramers via14 is allosterically hindering all-trans-retinol-dependent RBP4-TTR tertiary complex formation and that the compound could present ancillary therapeutic utility for indications treated with RBP4 antagonists, such as macular degeneration. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6HPLC of Formula: 82702-31-6).
Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.HPLC of Formula: 82702-31-6
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary