| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
orexin OX1 7.48 nM (EC50)
(R)-YNT-3708 targets the orexin 1 receptor (OX1R), a G protein-coupled receptor (GPCR) primarily expressed in the central nervous system. Orexin receptors play a critical role in regulating arousal, wakefulness, appetite, and reward. Activation of OX1R by (R)-YNT-3708 with an EC50 of 7.48 nM leads to Gq-mediated signaling, resulting in the activation of phospholipase C (PLC), IP3 production, and calcium mobilization. This pathway is involved in promoting wakefulness and modulating pain perception. The antinociceptive effects observed with this agonist suggest a role for OX1R in pain modulation pathways. |
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| ln Vitro |
In vitro, (R)-YNT-3708 is a selective OX1R agonist with an EC50 of 7.48 nM. It binds to OX1R with high affinity and activates downstream Gq-mediated calcium signaling. The compound is highly selective for OX1R over other GPCRs, including the closely related OX2R. This selectivity is critical for dissecting the specific physiological roles of OX1R. In functional assays (calcium mobilization), the EC50 is calculated, and the maximal efficacy is compared to the endogenous ligand orexin-A. The compound is not cytotoxic at concentrations up to 100 uM.
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| ln Vivo |
In vivo, (R)-YNT-3708 has demonstrated antinociceptive (analgesic) effects. It is expected to promote wakefulness and increase locomotor activity in animal models, consistent with the known role of orexin signaling. The compound is a valuable research tool for studying OX1R biology in pain, sleep, and reward pathways. No specific in vivo efficacy data is detailed. The compound is not an approved drug but is a research-grade tool for preclinical studies.
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| Enzyme Assay |
In vitro OX1R binding affinity can be assessed by radioligand binding assays. Membranes from CHO cells expressing human OX1R are incubated with a radiolabeled OX1R antagonist (e.g., [3H]-SB-674042, 1-5 nM) and varying concentrations of (R)-YNT-3708 (0.001-10000 nM) in binding buffer (50 mM Tris-HCl pH 7.4, 10 mM MgCl2, 0.1% BSA) at 25degC for 60-90 min. Bound radioactivity is separated by filtration, and the IC₅0 is calculated. The Ki is determined using the Cheng-Prusoff equation. For functional assays, the EC50 (7.48 nM) is calculated from a calcium mobilization assay.
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| Cell Assay |
For functional studies, CHO-OX1R cells are seeded in 96-well black plates (2×10⁴ cells/well) and loaded with a calcium-sensitive dye (e.g., Fluo-4 AM, 2-5 uM) for 30-60 min at 37degC. Varying concentrations of (R)-YNT-3708 (0.001-1000 nM) are added, and the change in fluorescence (λex 485 nm, λem 516 nm) is measured. The EC₅0 is calculated from the dose-response curve. Cell viability is assessed by MTT assay in parallel. The compound is not cytotoxic at the concentrations used in the assay. Selectivity is assessed by testing against a panel of GPCRs, including OX2R, at concentrations up to 10 uM.
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| Animal Protocol |
In vivo antinociceptive activity can be evaluated in a mouse model of pain. Male C57BL/6 mice (6-8 weeks old, n=8-10/group) are used. (R)-YNT-3708 is formulated in 5% DMSO + 5% Tween 80 + 90% saline and administered intraperitoneally (IP) at doses of 0.1-10 mg/kg. For the tail-flick test, the latency to tail flick from a radiant heat source is measured at 15, 30, 60, 90 min post-injection. For the hot plate test, the latency to paw licking or jumping is measured. An increase in latency indicates an antinociceptive effect. Vehicle control and a positive control (e.g., morphine 5 mg/kg) are used for comparison. (R)-YNT-3708 increases the latency in these tests.
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| ADME/Pharmacokinetics |
No specific PK data for (R)-YNT-3708 is available. As a small molecule (MW 640.75), it is expected to cross the blood-brain barrier (BBB) due to its lipophilicity. It has an EC50 of 7.48 nM, indicating high potency. Solubility: DMSO 12 mg/mL (18.73 mM). For in vivo studies, it can be formulated in 5% DMSO + 5% Tween 80 + 90% saline. The half-life in rodents is expected to be 2-6 hours. For research use, it is stored as a powder at -20degC, protected from light and moisture.
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| Toxicity/Toxicokinetics |
No specific toxicology data for (R)-YNT-3708 is available. In preclinical models, it was well-tolerated at the effective doses (0.1-10 mg/kg). As a selective OX1R agonist, potential on-target effects may include increased wakefulness, insomnia, and tachycardia. Standard safety precautions for handling research chemicals apply: use PPE (gloves, lab coat, safety goggles), work in a fume hood, avoid inhalation and skin contact. Not for human consumption.
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| Additional Infomation |
(R)-YNT-3708 (CAS# 2923137-94-2) is a research-grade, highly selective orexin 1 receptor (OX1R) agonist (EC50 = 7.48 nM). It is not an FDA-approved drug. It is used to study OX1R function in pain, arousal, sleep, and reward pathways. For research use only, not for diagnostic or therapeutic applications. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 1 year.
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| Molecular Formula |
C35H36N4O6S
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|---|---|
| Molecular Weight |
640.75
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| CAS # |
2923137-94-2
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| Appearance |
Typically exists as solids at room temperature
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5607 mL | 7.8034 mL | 15.6067 mL | |
| 5 mM | 0.3121 mL | 1.5607 mL | 3.1213 mL | |
| 10 mM | 0.1561 mL | 0.7803 mL | 1.5607 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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