YNT-185 di-HCl is a non-peptide, selective orexin type 2 receptor (OX2R) agonist/activator with EC50 of 0.028 and 2.75 μM for OX2R and OX1R respectively. YNT-185 di-HCl improves symptoms of episodic paralysis in a mouse model.

Physicochemical Properties

Molecular Formula	C33H39CL2N5O5S
Molecular Weight	688.664264917374
Exact Mass	687.204
CAS #	1804978-82-2
Related CAS #	YNT-185;1804978-81-1
PubChem CID	140307520
Appearance	Off-white to light yellow solid powder
Hydrogen Bond Donor Count	5
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	12
Heavy Atom Count	46
Complexity	1030
Defined Atom Stereocenter Count	0
SMILES	Cl.Cl.S(C1C(=CC=C(C2C=CC=C(C(N(C)C)=O)C=2)C=1)OC)(NC1C=CC=C(C=1)NCCNC(C1C=CC=CC=1N(C)C)=O)(=O)=O
InChi Key	AIORBDHFHVKRIY-UHFFFAOYSA-N
InChi Code	InChI=1S/C33H37N5O5S.2ClH/c1-37(2)29-15-7-6-14-28(29)32(39)35-19-18-34-26-12-9-13-27(22-26)36-44(41,42)31-21-24(16-17-30(31)43-5)23-10-8-11-25(20-23)33(40)38(3)4;;/h6-17,20-22,34,36H,18-19H2,1-5H3,(H,35,39);2*1H
Chemical Name	2-(dimethylamino)-N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]benzamide;dihydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	OX2 Receptor 0.028 μM (EC50) OX1 Receptor 2.75 μM (EC50)
ln Vivo	Mice treated with YNT-185 dihydrochloride (20–40 mg/kg; ip) show increased wakefulness[2]. In wild-type mice, but not in OXRDKO mice, YNT-185 dihydrochloride (300 nmol; icv) dose-dependently and dose-dependently increases wake time for three hours, accompanied by a reduction in NREM sleep time[2].
Animal Protocol	Animal/Disease Models: Male wild-type C57BL/6J mice[2] Doses: 20, 40 mg/kg Route of Administration: Ip Experimental Results: Wake time was also Dramatically increased.
References	[1]. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015;58(20):7931-7937. [2]. 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.

Solubility Data

Solubility (In Vitro)	DMSO: 125 mg/mL (181.51 mM) H2O: 100 mg/mL (145.21 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 12.5 mg/mL (18.15 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C). Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.4521 mL	7.2605 mL	14.5210 mL
	5 mM	0.2904 mL	1.4521 mL	2.9042 mL
	10 mM	0.1452 mL	0.7260 mL	1.4521 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.