BTRX-335140, formerly known as CYM-53093, a potent and selective KOR antagonist with IC50 (KOR)=0.8 nM. BTRX-335140 endowed with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments. orally administered CYM-53093 showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice. CYM-53093 exhibited a broad selectivity over a panel of off-target proteins. References: Guerrero M, Urbano M, Kim EK, Gamo Albero AM, Riley S, Abgaryan L, Leaf N, Van Orden LJ, Brown SJ, Xie J, Porreca F, Cameron MD, Rosen H, Roberts E. Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140). J Med Chem. 2019 Feb 1. doi: 10.1021/acs.jmedchem.8b01679. [Epub ahead of print] PubMed PMID: 30707578.

纯度：≥98%

CAS：2244614-14-8