4-me-pdtic

4-Me-PDTic is a potent and selective kappa opioid receptor antagonist.

4-Me-PDTic is a potent and selective Kappa Opioid Receptor Antagonist. 4-Me-PDTic had a Ke = 0.37 nM in a [35S]GTPγS binding assay and was 645- and >8100-fold selective for the κ relative to the μ and δ opioid receptors, respectively. Calculated logBB and CNS (central nervous system) multiparameter optimization (MPO) and low molecular weight values all predict that 4-Me-PDTic will penetrate the brain and pharmacokinetic studies in rats shows that 4-Me-PDTic does indeed penetrate the brain.

ETX0282 is an orally available, broad spectrum inhibitor of class A and C β-lactamases. Entasis is developing ETX0282 in combination with cefpodoxime proxetil, an orally available cephalosporin approved for treatment of a variety of bacterial infections.