YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC 50 s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models.
性状
Solid
IC50 & Target[1][2]
OX2 Receptor 0.028 μM (EC50) OX1 Receptor
体内研究(In Vivo)
YNT-185 dihydrochloride (20-40 mg/kg; i.p.) increases wakefulness in mice.
YNT-185 dihydrochloride (300 nmol; i.c.v.) significantly increases wake time for 3 hours in a dose-dependent manner, accompanied by a decrease in NREM sleep time, in wild-type mice but not in OXRDKO mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Nagahara T, et al. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015;58(20):7931-7937.[2]. 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.