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

TCN238 

Cat. No.: HY-14419 Purity: 98.31%
Handling Instructions

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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 73 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 116 In-stock
Estimated Time of Arrival: December 31
25 mg USD 248 In-stock
Estimated Time of Arrival: December 31
50 mg USD 429 In-stock
Estimated Time of Arrival: December 31
100 mg USD 748 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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

Molecular Weight

197.24

Formula

C12H11N3

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (760.49 mM)

*"≥" 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
10 mM 0.5070 mL 2.5350 mL 5.0700 mL
*Please refer to the solubility information to select the appropriate solvent.
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
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Product Name:
TCN238
Cat. No.:
HY-14419
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