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| 1mg |
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| Other Sizes |
| Targets |
PSB-1114 triethylamine targets the P2Y2 receptor, a member of the P2Y family of G protein-coupled receptors (GPCRs) that are activated by extracellular nucleotides. P2Y2 receptors are involved in various physiological processes, including inflammation, immune responses, and epithelial ion transport. The compound also shows selectivity for P2Y4 and P2Y6 receptors. It is a thio-substituted UTP analog with high enzymatic stability.
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| ln Vitro |
In vitro, PSB-1114 triethylamine is a potent and selective agonist of the P2Y2 receptor with an EC50 of 134 nM. It exhibits >50-fold selectivity for P2Y2 over P2Y4 (EC50 = 9.3 microM) and P2Y6 (EC50 = 7.0 microM) receptors. The compound is enzymatically stable due to its thio-beta,gamma-difluoromethylene modification, which protects it from degradation by ectonucleotidases. It is a valuable tool for studying P2Y2 receptor signaling in vitro.
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| ln Vivo |
In vivo, PSB-1114 triethylamine can be used to study the physiological roles of P2Y2 receptors in animal models. As a stable P2Y2 agonist, it is suitable for in vivo administration to investigate P2Y2-mediated effects on inflammation, airway epithelial function, and other processes. The compound is a potent, enzyme-stable, subtype-selective P2Y2 receptor agonist/activator with an EC50 of 134 nM.
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| Enzyme Assay |
A cell-free membrane binding assay is performed for P2Y2 receptor binding. Membranes from cells expressing recombinant human P2Y2 receptors (5-20 ug protein) are incubated with a radiolabeled P2Y2 agonist (e.g., [3⁵S]ATPalphaS or [3H]UTP, 0.5-2 nM) and increasing concentrations (0.1-10,000 nM) of PSB-1114 triethylamine in binding buffer. Bound radioligand is separated by filtration through GF/B filters. IC50 values are calculated, and Ki values are determined.
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| Cell Assay |
HEK293 cells stably expressing human P2Y2 receptors are seeded in 96-well plates. Cells are loaded with Fluo-4 AM (2-4 uM) for 30-60 min at 37degC. After washing, cells are pre-incubated in HBSS buffer. PSB-1114 triethylamine is added at varying concentrations (0.1-10,000 nM). Fluorescence (ex/em = 485/535 nm) is measured to monitor calcium flux. The EC50 for P2Y2 activation is calculated from the dose-response curve (reported EC50 = 134 nM). Control experiments using P2Y4- or P2Y6-expressing cells confirm selectivity.
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| Animal Protocol |
PSB-1114 triethylamine can be studied in mouse models of P2Y2 receptor function. C57BL/6 mice are used in models of airway inflammation or epithelial ion transport. The compound (0.1-10 mg/kg) is administered intraperitoneally or intratracheally. Lung function is assessed, and bronchoalveolar lavage fluid (BALF) is collected to measure inflammatory cell counts and cytokine levels (IL-6, TNF-alpha). P2Y2-mediated effects on airway surface liquid volume can be measured. The triethylamine salt form improves solubility for in vivo administration.
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| ADME/Pharmacokinetics |
PSB-1114 triethylamine has a logP of -4.6, indicating high hydrophilicity. The triethylamine salt form is used to enhance solubility. The compound is typically a solid at room temperature. It is stored at -20degC, sealed and protected from moisture. Specific PK parameters (t½, Cmax, AUC) have not been reported. The thio-beta,gamma-difluoromethylene modification confers enzymatic stability, likely prolonging its in vivo half-life.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are reported for PSB-1114 triethylamine. The compound is not a hazardous substance according to MSDS documentation. The triethylamine salt may cause mild irritation. Standard laboratory safety precautions should be followed. As a P2Y2 agonist, potential effects on inflammation and epithelial ion transport may occur at high doses. No formal toxicology studies have been published.
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| References | |
| Additional Infomation |
PSB-1114 triethylamine is a research-grade compound and is not approved for clinical use. It is a potent, enzyme-stable, subtype-selective P2Y2 receptor agonist (EC50 = 134 nM) that is >50-fold selective for P2Y2 over P2Y4 and P2Y6 receptors. The compound is a thio-substituted UTP analog and is a valuable research tool for studying P2Y2 receptor biology. This product is for research use only.
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| Molecular Formula |
C10H15F2N3O13P3S.XC6H15N
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| Related CAS # |
PSB-1114 tetrasodium;1657025-60-9
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| Appearance |
Light yellow to yellow solid powder
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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) |
H2O :≥ 100 mg/mL
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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.) |
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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