| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
OX2 Receptor 0.028 μM (EC50) OX1 Receptor 2.75 μM (EC50)
YNT-185 dihydrochloride targets the orexin type-2 receptor (OX2R) as a selective agonist. It has EC50 values of 0.028 μM for OX2R and 2.75 μM for OX1R, demonstrating approximately 100-fold selectivity for OX2R over OX1R. Orexin receptors are involved in the regulation of wakefulness, sleep-wake transitions, and appetite. By activating OX2R, YNT-185 promotes wake-promoting signaling pathways in the central nervous system. Its selectivity for OX2R makes it a valuable tool for studying the specific roles of this receptor in sleep-wake regulation and for developing treatments for narcolepsy. |
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| ln Vitro |
In vitro studies demonstrate that YNT-185 dihydrochloride is a nonpeptide, selective OX2R agonist with EC50 values of 0.028 μM for OX2R and 2.75 μM for OX1R. It activates OX2R with high potency and selectivity, promoting wake-promoting signaling pathways. The compound's nonpeptide nature and high selectivity make it a valuable tool for studying orexin receptor pharmacology and for developing small-molecule treatments for sleep disorders. Detailed in vitro characterization data, including receptor binding and functional assays, are available in the primary literature.
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| 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].
In vivo studies of YNT-185 dihydrochloride have demonstrated its efficacy in promoting wakefulness and suppressing cataplexy. In wild-type mice, YNT-185 (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. The compound suppresses cataplexy-like symptoms in OX knockout mice and ameliorates narcolepsy-cataplexy symptoms in mouse models. Its effects are mediated through OX2R activation, as no effects are observed in OXRDKO mice. These findings support the potential of YNT-185 for treating narcolepsy and other sleep disorders. |
| Enzyme Assay |
For OX2R binding assays, membrane preparations from cells expressing recombinant OX2R or OX1R are incubated with radiolabeled ligands and varying concentrations of YNT-185 dihydrochloride. Non-specific binding is determined using excess unlabeled reference compounds. Following incubation at appropriate temperature (typically 25°C for 60-90 minutes), bound and free radioligands are separated by rapid filtration through glass fiber filters. Filters are washed and radioactivity counted by liquid scintillation. IC50 or Ki values are calculated from competition curves. For functional assays, receptor activation is measured by calcium flux or IP3 accumulation assays.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing OX2R or OX1R (e.g., CHO or HEK293 cells) are cultured in appropriate media under standard conditions (37°C, 5% CO2). YNT-185 dihydrochloride is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Receptor activation is assessed by measuring intracellular calcium flux using fluorescent indicators or by measuring downstream signaling pathways. Cell viability and cytotoxicity can be assessed using standard assays. Each concentration is tested in replicate wells with vehicle controls and positive controls (e.g., orexin-A).
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| 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. For in vivo animal studies, YNT-185 dihydrochloride is typically administered via intracerebroventricular (i.c.v.) injection in mice. In wild-type mice, YNT-185 at 300 nmol significantly increases wake time for 3 hours in a dose-dependent manner, accompanied by a decrease in NREM sleep time. In OX knockout mice, the compound suppresses cataplexy-like symptoms. Sleep-wake parameters are monitored using EEG/EMG recordings. For pharmacokinetic studies, blood and brain tissue samples may be collected. All procedures must follow institutional animal care and use committee guidelines. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of YNT-185 dihydrochloride are characteristic of a small-molecule OX2R agonist. The compound has a molecular weight of 688.66 and formula C33H39Cl2N5O5S. CAS number: 1804978-82-2. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO and other organic solvents. As a nonpeptide agonist, it may have improved oral bioavailability compared to peptide-based orexin receptor agonists. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are reported in the primary literature.
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| Toxicity/Toxicokinetics |
According to available safety information, YNT-185 dihydrochloride is intended for research purposes only and is not for human use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist with EC50 values of 0.028 μM for OX2R and 2.75 μM for OX1R. It increases wake time in wild-type mice and suppresses cataplexy-like symptoms in OX knockout mice. The compound ameliorates narcolepsy-cataplexy symptoms in mouse models. It has a molecular weight of 688.66 and formula C33H39Cl2N5O5S. It is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C33H39CL2N5O5S
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|---|---|
| Molecular Weight |
688.664264917374
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| Exact Mass |
687.204
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| CAS # |
1804978-82-2
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| Related CAS # |
YNT-185;1804978-81-1
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| PubChem CID |
140307520
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
46
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
0
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| 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
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| InChi Key |
AIORBDHFHVKRIY-UHFFFAOYSA-N
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| 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
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| Chemical Name |
2-(dimethylamino)-N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]benzamide;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (181.51 mM)
H2O: 100 mg/mL (145.21 mM) |
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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