Price, Daniel J.; Drewry, David H.; Schaller, Lee T.; Thompson, Brian D.; Reid, Paul R.; Maloney, Patrick R.; Liang, Xi; Banker, Periette; Buckholz, Richard G.; Selley, Paula K.; McDonald, Octerloney B.; Smith, Jeffery L.; Shearer, Todd W.; Cox, Richard F.; Williams, Shawn P.; Reid, Robert A.; Tacconi, Stefano; Faggioni, Federico; Piubelli, Chiara; Sartori, Ilaria; Tessari, Michela; Wang, Tony Y. published the artcile< An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model>, Product Details of C19H34O2, the main research area is diarylazaindole pharmacokinetics blood brain barrier CAMKK2 AMPK satiety obesity; CAMKK2; Inhibitor; Satiety.
Hypothalamic CAMKK2 represents a potential mechanism for chem. affecting satiety and promoting weight loss in clin. obese patients. Single-digit nanomolar inhibitors of CAMKK2 were identified in three related ATP-competitive series. Limited optimization of kinase selectivity, solubility, and pharmacokinetic properties were undertaken on all three series, as SAR was often transferrable. Ultimately, a 2,4-diaryl 7-azaindole was optimized to afford a tool mol. that potently inhibits AMPK phosphorylation in a hypothalamus-derived cell line, is orally bioavailable, and crosses the blood-brain barrier. When dosed orally in rodents, compound 4t limited ghrelin-induced food intake.
Bioorganic & Medicinal Chemistry Letters published new progress about Antiobesity agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Product Details of C19H34O2.
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