TCN 238 |
| Catalog No.GC11501 |
Le TCN 238 est un modulateur allostérique positif (PAM) du récepteur mGlu4 biodisponible par voie orale avec une CE50 de 1 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 125404-04-8
Sample solution is provided at 25 µL, 10mM.
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TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
In the rat mGlu4 PAM in vitro assay the EC50 of TCN238 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].
TCN238 is highly CNS penetrant with a concentration of 33.8 μM in the brain. The plasma protein binding in rats is measured as 90% bound. The metabolic stability of TCN238 is assessed in rat and human microsomes and found to be 62% and 83% hepatic blood flow. The limited stability translated into a high in vivo clearance in rats of 75 mL/min/kg and TCN238 has a moderate volume of distribution (2.7 L/kg) with a short mean residence time (0.6 h) when dosed at 2 mg/kg via intravenous injection. TCN238 is orally bioavailable and 30 min following administration of a30 mg/kg dose, the plasma concentration is found to be 11.6 μM[1]. TCN 238 does not affect the performance of the learned task. However, the expression level of GRM4 in the hippocampus is reliable down-regulated five days after treatment with TCN 238. In addition, the expression level of GABRA1, encoding GABAA α-subunit is downregulated five days after the treatment in the frontal cortex[2].
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.
[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.
Animal experiment: | 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]. |
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. | |
| Cas No. | 125404-04-8 | SDF | |
| Chemical Name | (E)-4-styrylpyrimidin-2-amine | ||
| Canonical SMILES | NC1=NC=CC(/C=C/C2=CC=CC=C2)=N1 | ||
| Formula | C12H11N3 | M.Wt | 197.24 |
| Solubility | DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml,Ethanol: 5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.07 mL | 25.3498 mL | 50.6997 mL |
| 5 mM | 1.014 mL | 5.07 mL | 10.1399 mL |
| 10 mM | 507 μL | 2.535 mL | 5.07 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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