| Description | YNT-185 is a nonpeptide, selective agonist of the orexin type-2 receptor (OX2R), demonstrating EC50 values of 0.028 μM and 2.75 μM for OX2R and OX1R, respectively. Furthermore, YNT-185 effectively alleviates symptoms of narcolepsy-cataplexy in mouse models. |
| In vivo | YNT-185（20-40 mg/kg；i.p.）能够增强小鼠的警觉性。[1]。YNT-185（300 nmol；i.c.v.）以剂量依赖的方式显著延长了野生型小鼠的清醒时间达3小时，并伴随着非快速眼动（NREM）睡眠时间的减少，但在OXRDKO小鼠中无此效果。[1] |
| Target activity | OX1R:2.75 μM(EC50), OX2R:0.028(EC50) |
| molecular weight | 615.74 |
| Molecular formula | C33H37N5O5S |
| CAS | 1804978-81-1 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 62.0 mg/mL (90.0 mM) H2O: Insoluble |
| References | 1. Irukayama-Tomobe Y, et al. Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models. Proc Natl Acad Sci U S A. 2017;114(22):5731-5736. 2. Nagahara T, et al. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015;58(20):7931-7937. |