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YNT-185 Dihydrochloride Hydrate

for Cellbiology
Specification Assay :
98.0+% (HPLC)
Manufacturer :
FUJIFILM Wako Pure Chemical Corporation
Storage Condition :
Keep at -20 degrees C.
CAS RN® :
1804978-82-2
Molecular Formula :
C33H37N5O5S・2HCl・nH2O
Molecular Weight :
688.66(
  • Structural Formula
  • Label
  • Packing
SDS
Comparison
Product Number
Package Size
Price
Inventory
Distributor
254-00641
Barcode No
4548995053152
5mg
List Price
154.00 USD

In stock in Japan

Distributor
250-00643
Barcode No
4548995053169
100mg
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Out of Stock

Document

SDS
Product Specification Sheet
Spectral Data
Certificate of Analysis
Calibration Certificate

Overview

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.

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  • Appearance: White ~ slightly light brown, crystalline powder ~ powder
  • Content (HPLC): 98.0% or more
  • Solubility: Physiological saline (pH 2.4) ... 1.3 mol/L1)
    ※ The optimum pH when dissolving is about 2.4 or less.
  • 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 RN® : 1804978-82-2 (anhydride)

Wake-Promoting Effect

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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)

References

  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).
  2. Irukayama-Tomobe, Y., Ogawa, Y., Tominaga, H., Ishikawa, Y., Hosokawa, N., Ambai, S., Kawabe, Y., Uchida, S., Nakajima, R., Saitoh, T., Kanda, T., Vogt, K., Sakurai, T., Nagase, H. and Yanagisawa, M. : Proc. Natl. Acad. Sci. USA, 114(22), 573(2017).
  3. Toyama, S., Shimoyama, N., Tagaito, Y., Nagase, H., Saitoh, T., Yanagisawa, M. and Shimoyama, M. : Anesthesiology, 128, 992 (2018).
  4. Yamamoto, K., Okui, R. and Yamatodani, A. : Naunyn Schmiedebergs Arch. Pharmacol. (2019). doi: 10.1007/s00210-019-01646-x.

Property

Appearance White - slightly brown, crystalline powder - powder

Manufacturer Information

Alias

  • YNT-185・2HCl
    3'-{{{3-{{2-{[2-(Dimethylamino)benzoyl]amino}ethyl}amino}phenyl}amino}sulfonyl}-4'-methoxy-N,N-dimethyl-(1,1'-biphenyl)-3-carboxamide Dihydrochloride Hydrate

For research use or further manufacturing use only. Not for use in diagnostic procedures.

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