| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
PYD-106 selectively targets NMDA receptors that contain the GluN2C subunit. It acts as a positive allosteric modulator (PAM) at these receptors. The compound has an EC50 of 13 µM for enhancing the maximal current response of GluN1/GluN2C receptors. It enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors, demonstrating a high degree of subunit selectivity.
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| ln Vitro |
In vitro, PYD-106 selectively enhances the activity of GluN2C-containing NMDA receptors. It increases the opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist. It has a modest effect on the EC50 of glutamate and glycine. The compound enhances glutamate-induced maximal current responses in HEK293 cells expressing NR1/NR2C NMDA receptors with an EC50 of 13 µM. This selective modulation is a key feature of its activity.
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| ln Vivo |
In vivo, the activity of PYD-106 is expected to be related to its modulation of GluN2C-containing NMDA receptors. These receptors are implicated in various neurological and psychiatric disorders. However, specific in vivo data for PYD-106 is not detailed in the available literature. Its use as a research tool suggests that it has been used to study the physiological and pathophysiological roles of GluN2C-containing NMDA receptors in animal models.
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| Enzyme Assay |
Cell-free assays for PYD-106 are not the primary method for characterizing its activity, as it is a positive allosteric modulator (PAM) whose function depends on the presence of the receptor. The most relevant assays involve the use of membrane preparations from cells expressing the receptor, but these are still cellular assays. Cell-free methods might include radioligand binding studies to determine if the compound competes with known ligands for the glutamate or glycine binding sites, but PYD-106 has only modest effects on glutamate and glycine EC50, suggesting it does not bind to these sites.
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| Cell Assay |
In vitro cell-based assays for PYD-106 are performed to measure its activity as a positive allosteric modulator. A common method is the whole-cell patch-clamp electrophysiology technique. HEK293 cells are transfected to express specific NMDA receptor subtypes, such as NR1/NR2C. The cells are then voltage-clamped, and currents are evoked by the application of agonists like glutamate and glycine. PYD-106 is co-applied, and the potentiation of the evoked current is measured. The EC50 for potentiation is calculated from a dose-response curve. This assay directly demonstrates the compound's modulatory effect.
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| Animal Protocol |
In vivo animal experiments for PYD-106 would be designed to study the function of GluN2C-containing NMDA receptors in the brain. For example, the compound could be administered to rodents, and its effect on behaviors related to NMDA receptor function, such as learning, memory, and sensorimotor gating, could be assessed. It could also be used in disease models where GluN2C receptors are implicated. Specific protocols for PYD-106 are not detailed in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for PYD-106 is not provided in the available literature. Its properties, such as oral bioavailability, half-life, and brain penetration, would be important for its use as an in vivo research tool. For storage, the compound is typically kept as a powder at -20°C for up to three years.
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| Toxicity/Toxicokinetics |
Toxicological data for PYD-106 is not available in the public literature. As a research compound that modulates NMDA receptor function, its safety profile would be a critical consideration. However, no specific LD50, organ toxicity, or genotoxicity data are reported. Its use is strictly for research purposes, and it is not intended for human therapeutic use.
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| Additional Infomation |
PYD-106 is a research-grade compound used as a selective tool to study the function of GluN2C-containing NMDA receptors. Its high selectivity for these receptors over other NMDA receptor subtypes makes it invaluable for dissecting their unique roles in the brain. It is particularly useful for studying the physiology and potential therapeutic targeting of GluN2C in conditions like schizophrenia and other neurological disorders. It has not been approved for clinical use. All information is for research reference and not for diagnostic or clinical use.
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| Molecular Formula |
C25H24N2O5
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|---|---|
| Molecular Weight |
432.476
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| Exact Mass |
432.168
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| CAS # |
1560894-05-4
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| PubChem CID |
90035858
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
723.0±60.0 °C at 760 mmHg
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| Flash Point |
391.0±32.9 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.663
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| LogP |
3.45
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
785
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C(N(CCC2=C(C)NC3C=CC=CC2=3)C(C2C=CC(C(=O)OC)=CC=2)C=1C(C)=O)=O
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| InChi Key |
LIFGURQFZLMSDE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24N2O5/c1-14-18(19-6-4-5-7-20(19)26-14)12-13-27-22(21(15(2)28)23(29)24(27)30)16-8-10-17(11-9-16)25(31)32-3/h4-11,22,26,29H,12-13H2,1-3H3
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| Chemical Name |
methyl 4-[3-acetyl-4-hydroxy-1-[2-(2-methyl-1H-indol-3-yl)ethyl]-5-oxo-2H-pyrrol-2-yl]benzoate
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| Synonyms |
PYD106; PYD 106; PYD-106
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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 | 2.3122 mL | 11.5612 mL | 23.1225 mL | |
| 5 mM | 0.4624 mL | 2.3122 mL | 4.6245 mL | |
| 10 mM | 0.2312 mL | 1.1561 mL | 2.3122 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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