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Non-peptide Orexin 2 Receptor Agonist
YNT-185・2HCl

YNT-185·2HCl is non-peptide orexin receptor 2 (OX2R) agonist.   Orexins are a family of neuropeptides, which are secreted by orexin-producingnerve present in the hypothalamus.  There are two variants, orexin receptors exist as two types of receptors, type 1 and type 2.  In particular, the orexin 2 receptor is involved in sleep-wake regulation, and orexin deficiency in the brain causes narcolepsy, a sleep disorder manifesting as an unbearable sleepiness during the day.  Although it has been reported that intraventricular administration of orexin leads to symptom alleviation in narcolepsy mouse models, therapeutic effects cannot be expected unless it is administered into the brain, due to orexin being a peptide and being unable to pass through the blood-brain barrier.  Intraventricular or intraperitoneal administration of YNT-185·2HCl has been shown to extend wake time, and has also been reported to improve the symptoms of narcolepsy mouse models.


1. Link



Leaflet
Leaflet

Package Insert

2. Product Outline

    YNT-185・2HCl
  • Appearance: White ~ slightly pale brown, crystalline powder ~ powder
  • Assay (HPLC): 98.0+ %
  • Solubility: Saline (pH 2.4*)・・・ 1.3 mol/L 1)
     * Optimum pH (after dissolving): ≤ approx. 2.4
  • EC50: OX2R ··· 0.028 μmol/L (free base)1)
              OX1R ··· 2.750 μmol/L (free base)1)
  • C33H37N5O5S·2HCl·nH2O (C33H37N5O5S·2HCl = 688.66)
  • CAS No. 1804978-82-2 (anhydride)

3. Data: Wake-Promoting Effect

Wake-Promoting Effect

When YNT-185·2HCl was intracerebroventricularly administered in mouse, volume-dependent increase of awaking level was shown.  No awaking effect was observed in orexin-deficient mice. From this, it was confirmed that YNT-185・2HClhas an effect on orexin receptors.
(Data was provided by Yanagisawa M., Nagase H. and Funato H. at International Institute for Integrative Sleep Medicine (WPI-IIIS), University of Tsukuba)

4. Reference

  1. Nagahara, T., Saitoh, T., Kutsumura, N., Irukayama-Tomobe, Y., Ogawa, Y., Kuroda, D., Gouda, H., Kumagai, H., Fujii, H., Yanagisawa, M. and Nagase, H. : J. Med. Chem., 58, 7931 (2015).

5. Product List

Product Name Package Size Wako Cat. No. Grade Storage Condition
YNT-185 Dihydrochloride Hydrate 5 mg 254-00641 for Cellbiology Keep at -20°C.
100 mg 250-00643

6. Related Products

Product Name Package Size Wako Cat. No. Grade Storage Condition
Orexins
Orexin A(Human) 0.1 mg 159-03161 for Cellbiology Keep at -20°C.
Orexin B(Human) 0.1 mg 156-03171
Orexin B(Rat, Mouse) 0.1 mg 153-03181
Orexin Receptor Agonists
[Ala11, D-Leu15]-Orexin B 1 mg 013-24771 for Cellbiology Keep at -20°C.
SB-668875 1 mg 194-17221
Orexin Receptor Antagonists
JNJ 10397049 10 mg 104-00171 for Cellbiology Keep at 2 - 10°C.
50 mg 100-00173
250 mg 108-00174
SB-408124 5 mg 196-17421 Keep at -20°C.
25mg 192-17423
SB-674042 5 mg 192-17761
25 mg 198-17763

Home > Products > Life Science > Disease Research > YNT-185·2HCl
Home > Products > Life Science > Physiological Active Substances > YNT-185·2HCl