| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
YNT-185 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 specifically 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 sleep disorders such as narcolepsy.
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| ln Vitro |
In vitro studies demonstrate that YNT-185 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 exposed to YNT-185 (20–40 mg/kg; ip) become more awake[2]. In wild-type mice, but not in OXRDKO mice, YNT-185 (300 nmol; icv) dramatically lengthens wake time for three hours in a dose-dependent manner, concomitant with a reduction in NREM sleep time[2].
In vivo studies of YNT-185 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. 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 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 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 are characteristic of a small-molecule OX2R agonist. The compound has a molecular weight of 615.74 and formula C33H37N5O5S. CAS number: 1804978-81-1. 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 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 |
selective agonists of orexin type 2 receptor (OX2R)
YNT-185 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 mouse models. It has a molecular weight of 615.74 and formula C33H37N5O5S. It is for research use only with no clinical development or regulatory approvals reported. |
| Molecular Formula |
C33H37N5O5S
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| Molecular Weight |
615.74
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| Exact Mass |
615.251
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| CAS # |
1804978-81-1
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| Related CAS # |
YNT-185 dihydrochloride;1804978-82-2
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| PubChem CID |
122192250
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
44
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C2=CC=C(OC)C(S(NC3=CC=CC(NCCNC(=O)C4=CC=CC=C4N(C)C)=C3)(=O)=O)=C2)=CC=CC(C(N(C)C)=O)=C1
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| InChi Key |
BXJSAMKIFDDLGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H37N5O5S/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)
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| Chemical Name |
2-(dimethylamino)-N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]benzamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 100 mg/mL (162.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6241 mL | 8.1203 mL | 16.2406 mL | |
| 5 mM | 0.3248 mL | 1.6241 mL | 3.2481 mL | |
| 10 mM | 0.1624 mL | 0.8120 mL | 1.6241 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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