| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Methoxy-PEPy specifically targets the metabotropic glutamate receptor 5 (mGlu5), a G protein-coupled receptor involved in synaptic transmission and plasticity. It acts as a negative allosteric modulator, binding to a site distinct from the orthosteric binding site and inhibiting receptor activation. The compound is a highly efficient and selective inhibitor with an IC50 of 1 nM. Its high potency and selectivity make it a valuable tool for studying mGlu5 receptor function in neurological research.
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| ln Vitro |
In vitro, Methoxy-PEPy demonstrates potent and selective inhibition of the mGlu5 receptor with an IC50 of 1 nM. The compound is a small-molecule antagonist used in pharmacological research to study mGlu5 receptor function. It is soluble in DMSO (100 mg/mL with ultrasonic assistance). Methoxy-PEPy's high selectivity for mGlu5 over other glutamate receptors makes it a valuable tool for studying mGlu5-mediated signaling pathways. Its potency has been characterized in various receptor binding and functional assays.
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| ln Vivo |
In vivo, Methoxy-PEPy has been studied for its effects on mGlu5 receptor-mediated behaviors and neurological functions. As a potent and selective mGlu5 antagonist, it is used in preclinical research to investigate the role of mGlu5 in various neurological and psychiatric disorders. The compound's high potency (IC50 = 1 nM) suggests potential for in vivo efficacy. Further in vivo studies are ongoing to fully characterize its pharmacokinetic and pharmacodynamic properties. The compound is typically administered orally or via injection in preclinical studies.
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| Enzyme Assay |
Methoxy-PEPy receptor binding assays involve measuring affinity for the mGlu5 receptor. Radioligand binding displacement studies are performed using membranes from cells expressing recombinant mGlu5 receptors. The compound's IC50 of 1 nM is determined through competitive binding assays. Functional antagonism is assessed by measuring inhibition of mGlu5-mediated signaling such as calcium mobilization or inositol phosphate accumulation. Selectivity is confirmed by testing against other glutamate receptor subtypes. Assays are performed in appropriate buffer systems with positive controls such as known mGlu5 antagonists (e.g., MPEP).
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| Cell Assay |
Methoxy-PEPy cell-based assays are conducted in cells expressing recombinant mGlu5 receptors. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Methoxy-PEPy at varying concentrations. mGlu5 receptor activation is assessed by measuring calcium mobilization using fluorescent calcium indicators or by measuring downstream signaling pathways. The compound's IC50 of 1 nM is confirmed through functional assays. Cell viability is assessed by standard assays. Selectivity is confirmed by testing against other glutamate receptor subtypes. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
Methoxy-PEPy in vivo studies are conducted in rodent models of neurological and psychiatric disorders. Animals are treated with Methoxy-PEPy via oral administration or injection. Behavioral tests such as locomotor activity, anxiety-like behavior, and cognitive function are assessed. For receptor occupancy studies, animals are treated with Methoxy-PEPy and receptor occupancy is measured using PET imaging or ex vivo binding assays. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs. Tissues and blood samples are collected for biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Methoxy-PEPy (MW 210.23 g/mol, C13H10N2O) is a small molecule mGlu5 antagonist. It is soluble in DMSO (100 mg/mL with ultrasonic assistance). The compound is stable as a powder at -20°C for up to 3 years and at 4°C for 2 years. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. The compound is typically used in neurological research for studying mGlu5 receptor function.
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| Toxicity/Toxicokinetics |
Methoxy-PEPy is generally well-tolerated in preclinical studies. The compound is a potent and selective mGlu5 antagonist with an IC50 of 1 nM. Its high potency and selectivity suggest a favorable safety profile for research applications. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References |
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| Additional Infomation |
Methoxy-PEPy is a potent and selective negative allosteric modulator of the metabotropic glutamate receptor 5 (mGlu5) with an IC50 of 1 nM. It is used in pharmacological research to study mGlu5 receptor function and related signaling pathways. The compound's high potency and selectivity make it a valuable tool for neurological research. Methoxy-PEPy is also known as 3-methoxy-5-(2-pyridinylethynyl)pyridine. All applications are limited to non-human research use.
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| Molecular Formula |
C13H10N2O
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|---|---|
| Molecular Weight |
210.231
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| Exact Mass |
210.079
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| CAS # |
524924-76-3
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| PubChem CID |
10081842
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| Appearance |
Yellow to green solid powder
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| LogP |
1.885
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
278
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VRTFKUFTEWQHDD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10N2O/c1-16-13-8-11(9-14-10-13)5-6-12-4-2-3-7-15-12/h2-4,7-10H,1H3
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| Chemical Name |
3-methoxy-5-(2-pyridin-2-ylethynyl)pyridine
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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) |
DMSO : ~100 mg/mL (~475.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7567 mL | 23.7835 mL | 47.5670 mL | |
| 5 mM | 0.9513 mL | 4.7567 mL | 9.5134 mL | |
| 10 mM | 0.4757 mL | 2.3783 mL | 4.7567 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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