《Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor》 was written by Bartolini, Desiree; De Franco, Francesca; Torquato, Pierangelo; Marinelli, Rita; Cerra, Bruno; Ronchetti, Riccardo; Schon, Arne; Fallarino, Francesca; De Luca, Antonella; Bellezza, Guido; Ferri, Ivana; Sidoni, Angelo; Walton, William G.; Pellock, Samuel J.; Redinbo, Matthew R.; Mani, Sridhar; Pellicciari, Roberto; Gioiello, Antimo; Galli, Francesco. Recommanded Product: 21085-72-3 And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
Pregnane X receptor (PXR) is a master xenobiotic-sensing transcription factor and a validated target for immune and inflammatory diseases. The identification of chem. probes to investigate the therapeutic relevance of the receptor is still highly desired. In fact, currently available PXR ligands are not highly selective and can exhibit toxicity and/or potential off-target effects. In this study, we have identified garcinoic acid as a selective and efficient PXR agonist. The properties of this natural mol. as a specific PXR agonist were demonstrated by the screening on a panel of nuclear receptors, the assessment of the phys. and thermodn. binding affinity, and the determination of the PXR-garcinoic acid complex crystal structure. Cytotoxicity, transcriptional, and functional properties were investigated in human liver cells, and compound activity and target engagement were confirmed in vivo in mouse liver and gut tissue. In conclusion, garcinoic acid is a selective natural agonist of PXR and a promising lead compound toward the development of new PXR-regulating modulators. The experimental part of the paper was very detailed, including the reaction process of (2R,3R,4S,5S,6S)-2-Bromo-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate(cas: 21085-72-3Recommanded Product: 21085-72-3)
(2R,3R,4S,5S,6S)-2-Bromo-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate(cas: 21085-72-3) may be used for the synthesis of HMR1098-S-Glucuronide Methyl Ester, a new K-ATP-blocking agent being developed as a drug for prevention of sudden cardiac death.Recommanded Product: 21085-72-3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary