R-PSOP (C09-1167-584)

R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the K i s of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders.In VitroFrom Schild analyses, the functional K b values for R-PSOP are 92 and 155 nM at human and rat NMUR2, respectively (the effects of R-PSOP on the intracellular calcium mobilization response induced by NMU-25 in HEK293 cells expressing human or rat NMUR2). R-PSOP strongly inhibits the responses stimulated by peptide agonists NMU-25, NMU-23, and NMU-8 in human embryonic kidney 293 cells expressing NMUR2. In functional assays measuring phosphoinositide turnover or intracellular calcium mobilization, R-PSOP strongly inhibits the responses stimulated by peptide agonists NMU-25, NMU-23, and NMU-8 in human embryonic kidney 293 cells expressing NMUR2. R-PSOP concentration-dependently inhibits the phosphoinositide (PI) turnover turnover response in human NMUR2-expressing cells stimulated by 10 nM NMU-25 (EC 50 of 5 nM). The IC 50 value is determined to be 86 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoR-PSOP (10 μL 50 nmol; intrathecal injection; male Sprague-Dawley rats) attenuates NMU-23-evoked nociceptive responses in a rat spinal reflex preparation . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:Solid. Specifications and Purity: 99%. Molecular Formula: C20H22N4O2. Molecular Weight: 350.41.