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TG6-129

Name: TG6-129
Brand: TargetMol
SKU: T28958
Price: 123 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T28958Cas No. 1164464-14-5

Alias TG6 129

TG6-129 is an antagonist of the EP2 receptor. TG6-129 suppresses PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM. TG6-129 reduces the expression of COX-2, IL-1β, IL-6, IL-12, IL-23 and TNF-α induced by the EP2-selective agonist butaprost in P388D1 macrophages.

TG6-129

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Purity: 99.55%

Catalog No. T28958Alias TG6 129Cas No. 1164464-14-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$123	In Stock	In Stock
5 mg	$253	In Stock	In Stock
10 mg	$449	In Stock	In Stock
25 mg	$739	In Stock	In Stock
50 mg	$987	In Stock	In Stock
100 mg	$1,390	In Stock	In Stock
500 mg	$2,820	-	In Stock
1 mL x 10 mM (in DMSO)	$357	In Stock	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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Purity:99.55%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

TG6-129 AI Summary

TG6-129 exhibits a comprehensive profile of bioactivities across various biological targets and systems. It acts as an antagonist at multiple prostanoid receptors, including EP2 (Kb = 8.8 nM), EP4 (Kb = 3900.0 nM), DP1 (Kb = 14600.0 nM), and IP (Kb = 199.0 nM) receptors, demonstrating selective inhibitory effects. The compound shows good metabolic stability in mouse and human liver microsomes, with 40% remaining activity after 60 minutes at concentrations of 1 to 10 µM. It also has a moderate plasma concentration (30.0 µM at 5 mg/kg and 12.0 µM at 10 mg/kg) in mice and exhibits aqueous solubility of 71.0 µg/mL in PBS buffer at pH 7.0. Notably, the compound has low brain penetration with a brain-to-plasma ratio of 0.02 at 10 mg/kg. In terms of cellular effects, TG6-129 has a cytotoxicity value (CC50) of 326,000 nM against rat C6 cells after 48 hours, indicating its toxicity levels. It inhibits the human EP2 receptor in rat C6 cells with an IC50 of 1600 nM against PGE2-induced cAMP accumulation and shows inhibitory activity against Staphylococcus aureus NadD with an IC50 of 4500 nM. Additionally, the compound has been found to affect beta-arrestin recruitment assays across various GPCR targets, showing percentage inhibitions ranging from -8.355% to -64.44%, suggesting a complex activity profile in GPCR signaling pathways. It also modulates thermal stability in different protein domains, indicating varied effects on protein interactions. Overall, TG6-129 holds potential as a versatile biological modulator, with significant activities in receptor antagonism, antimicrobial properties, and effects on protein stability and cell viability..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	TG6-129 is an antagonist of the EP2 receptor. TG6-129 suppresses PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM. TG6-129 reduces the expression of COX-2, IL-1β, IL-6, IL-12, IL-23 and TNF-α induced by the EP2-selective agonist butaprost in P388D1 macrophages.
Synonyms	TG6 129

Chemical Properties

Molecular Weight	491.58
Formula	C₂₀H₁₈FN₅O₃S₃
Cas No.	1164464-14-5
Smiles	CCC1=NN=C(NS(=O)(=O)C2=CC=C(NC(=S)NC(=O)\C=C\C3=CC=C(F)C=C3)C=C2)S1
Relative Density.	1.518 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: 55 mg/mL (111.88 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0343 mL	10.1713 mL	20.3426 mL	101.7128 mL
5 mM	0.4069 mL	2.0343 mL	4.0685 mL	20.3426 mL
10 mM	0.2034 mL	1.0171 mL	2.0343 mL	10.1713 mL
20 mM	0.1017 mL	0.5086 mL	1.0171 mL	5.0856 mL
50 mM	0.0407 mL	0.2034 mL	0.4069 mL	2.0343 mL
100 mM	0.0203 mL	0.1017 mL	0.2034 mL	1.0171 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