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TC-N 22A

Name: TC-N 22A
Brand: TargetMol
SKU: T23440
Price: 123 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T23440Cas No. 1314140-00-5

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

TC-N 22A

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Purity: 99.95%

Catalog No. T23440Cas No. 1314140-00-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$123	In Stock	In Stock
5 mg	$263	In Stock	In Stock
10 mg	$325	In Stock	In Stock
25 mg	$548	In Stock	In Stock
50 mg	$788	In Stock	In Stock
100 mg	$1,080	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.95%

Appearance:Solid

Color:Orange

Resource Download

COA HNMR LCMS

Product Introduction

TC-N 22A AI Summary

TC-N 22A exhibits diverse bioactivities, including high plasma protein binding in both rats and humans, suggesting a strong affinity for protein binding. It acts as a positive allosteric modulator of the human mGlu4 receptor, enhancing glutamate-induced responses. The compound has moderate lipophilicity with a LogD value of 5.0 and demonstrates potent drug uptake in the rat brain, maintaining a favorable brain-to-plasma ratio post oral administration. Its high permeability is consistent across PAMPA and MDCK cell assays, although it shows a moderate efflux ratio in P-gp substrate assays, indicating potential substrate functionality. TC-N 22A shows high solubility at pH 7.4 and even higher at pH 1.5 and has an IC50 value of 28000.0 nM for inhibiting human ERG. It also displays intrinsic clearance in rat hepatocytes with a broad clearance rate range, exemplified by a specific rate of 36.31 uL.min^-1.(10^6 cells)^-1. The compound's effects on cell viability and growth rates are cell-type-specific, reducing growth in HEK293T cells but showing variable effects on U2OS cells and human fibroblasts. Thermal Shift Assays highlight its impact on protein stability, inducing changes in the melting temperatures of protein domains, implying complex interaction profiles. In GPCR beta-arrestin recruitment assays, TC-N 22A functions as an agonist for FFAR4, GPR35, APLNR, ADGRF1, and S1PR1, with partial agonistic activity on GLP1R. It also exhibits antagonist effects on multiple targets including FFAR4, GPR35, APLNR, ADRA2A, GPR119, FPR2, ADRB2, CX3CR1, GLP1R, AGTR1, ADGRF1, S1PR1, and C5AR1, underscoring its broad receptor modulatory capabilities..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

Targets&IC50

mGlu1/2/3/5/7 receptors:>10 μM (EC50), mGluR4:9 nM (EC50)

Chemical Properties

Molecular Weight	283.35
Formula	C₁₄H₁₃N₅S
Cas No.	1314140-00-5
Smiles	N(C1=NC=2C=3C(=NNC3)CCCC2S1)C4=CC=CC=N4
Relative Density.	1.435 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (176.46 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.5292 mL	17.6460 mL	35.2920 mL	176.4602 mL
5 mM	0.7058 mL	3.5292 mL	7.0584 mL	35.2920 mL
10 mM	0.3529 mL	1.7646 mL	3.5292 mL	17.6460 mL
20 mM	0.1765 mL	0.8823 mL	1.7646 mL	8.8230 mL
50 mM	0.0706 mL	0.3529 mL	0.7058 mL	3.5292 mL
100 mM	0.0353 mL	0.1765 mL	0.3529 mL	1.7646 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc