2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. TCN238

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.

TCN238 Chemical Structure

TCN238 Chemical Structure

CAS No. : 125404-04-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 116 In-stock
25 mg USD 248 In-stock
50 mg USD 429 In-stock
100 mg USD 748 In-stock
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Based on 1 publication(s) in Google Scholar

TCN238 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM[1].

IC50 & Target[1]

mGlu4 Receptor

1 μM (EC50)

In Vitro

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.

TCN238 Related Antibodies
In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

197.24

Formula

C12H11N3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC=CC(/C=C/C2=CC=CC=C2)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (760.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.0700 mL 25.3498 mL 50.6997 mL
5 mM 1.0140 mL 5.0700 mL 10.1399 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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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TCN238 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TCN238125404-04-8TCN 238TCN-238mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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