TCN238
Based on 1 Customer Validation
TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 125404-04-8
- Formula: C12H11N3
- Molecular Weight:197.24
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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mGlu4 Receptor 1 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
>10 μM
Compound: 11
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Agonist activity at human mGluR5 expressed in CHO-K1 cells in absence of glutamate
Agonist activity at human mGluR5 expressed in CHO-K1 cells in absence of glutamate
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[PMID: 20638279] |
| CHO-K1 | EC50 |
>10 μM
Compound: 11
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Positive allosteric modulation of human mGluR5 expressed in CHO-K1 cells
Positive allosteric modulation of human mGluR5 expressed in CHO-K1 cells
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[PMID: 20638279] |
| CHO-K1 | EC50 |
>30 μM
Compound: 11
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Agonist activity at human mGluR4 expressed in CHO-K1 cells
Agonist activity at human mGluR4 expressed in CHO-K1 cells
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[PMID: 20638279] |
| CHO-K1 | EC50 |
1 μM
Compound: 11
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Positive allosteric modulation of human mGluR4 expressed in CHO-K1 cells assessed as decrease in forskolin-induced intracellular cAMP accumulation after 1 hr by fluorescence assay
Positive allosteric modulation of human mGluR4 expressed in CHO-K1 cells assessed as decrease in forskolin-induced intracellular cAMP accumulation after 1 hr by fluorescence assay
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[PMID: 20638279] |
| CHO-K1 | EC50 |
1 μM
Compound: 11
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Positive allosteric modulation of rat mGluR4 expressed in CHO-K1 cells
Positive allosteric modulation of rat mGluR4 expressed in CHO-K1 cells
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[PMID: 20638279] |
| CHO-K1 | IC50 |
>10 μM
Compound: 11
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Negative allosteric modulation of rat mGluR5 expressed in CHO-K1 cells
Negative allosteric modulation of rat mGluR5 expressed in CHO-K1 cells
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[PMID: 20638279] |
| CHO-K1 | IC50 |
>30 μM
Compound: 11
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Negative allosteric modulation of human mGluR5 expressed in CHO-K1 cells
Negative allosteric modulation of human mGluR5 expressed in CHO-K1 cells
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[PMID: 20638279] |
In the rat mGlu4 PAM in vitro assay the EC50 of TCN238 (Compound 11) is 1 μM which is comparable to the human assay. TCN238 is screened in rat and human mGlu5 assays, the IC50 of 11 is >30 μM on human mGlu5and >10 μM on rat mGlu5. TCN238 is run in a receptor screening panel of 68 targets and no activity is observed at ≥50% at 10 μM for any of the receptors. In CaCo-2 cells, TCN238 is found to have good permeability with no apparent efflux issue[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 125404-04-8
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Appearance Solid
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Molecular Weight 197.24
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Formula C12H11N3
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Color White to off-white
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SMILES
NC1=NC=CC(/C=C/C2=CC=CC=C2)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (507.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Rats: TCN 238 is administered subcutaneously at a dose of 2 mg/kg (volume of 0.5 mL) four times in two days (morning and evening). Retrieval of the task is tested 30min after the first and third injections of TCN 238, and 5 days after the last injection of the substance. During the retrieval test the animals are placed to the start box, the door is opened, and the latent period of response is registered.[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. East SP, et al. An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4901-5. [Content Brief]
[2]. Pershina EV, et al. Subacute activation of mGlu4 receptors causes the feedback inhibition of its gene expression in rat brain. Life Sci. 2016 May 15;153:50-4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.0700 mL | 25.3498 mL | 50.6997 mL | 126.7491 mL |
| 5 mM | 1.0140 mL | 5.0700 mL | 10.1399 mL | 25.3498 mL | |
| 10 mM | 0.5070 mL | 2.5350 mL | 5.0700 mL | 12.6749 mL | |
| 15 mM | 0.3380 mL | 1.6900 mL | 3.3800 mL | 8.4499 mL | |
| 20 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL | 6.3375 mL | |
| 25 mM | 0.2028 mL | 1.0140 mL | 2.0280 mL | 5.0700 mL | |
| 30 mM | 0.1690 mL | 0.8450 mL | 1.6900 mL | 4.2250 mL | |
| 40 mM | 0.1267 mL | 0.6337 mL | 1.2675 mL | 3.1687 mL | |
| 50 mM | 0.1014 mL | 0.5070 mL | 1.0140 mL | 2.5350 mL | |
| 60 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1125 mL | |
| 80 mM | 0.0634 mL | 0.3169 mL | 0.6337 mL | 1.5844 mL | |
| 100 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2675 mL |
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