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TGR5 Receptor Agonist

Name: TGR5 Receptor Agonist
Brand: TargetMol
SKU: T1824
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1824Cas No. 1197300-24-5

TGR5 is a potent TGR5(GPCR19) agonist.

TGR5 Receptor Agonist

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Purity: 99.93%

Catalog No. T1824Cas No. 1197300-24-5

TGR5 is a potent TGR5(GPCR19) agonist.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
5 mg	$79	In Stock	In Stock
10 mg	$133	In Stock	In Stock
25 mg	$263	In Stock	In Stock
50 mg	$463	In Stock	In Stock
100 mg	$693	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$88	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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Batch Information

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Purity:99.93%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	TGR5 is a potent TGR5(GPCR19) agonist.
Targets&IC50	TGR5/GPCR19 (melanophore cells):7.5(pEC50), TGR5/GPCR19 (U2-OS cells):6.8(pEC50)
Kinase Assay	Inhibition assays are carried out in 384-well white ProxiPlates in 10 μL of reaction volume. Standard reaction mixtures consisted of the compound (in 2% DMSO final concentration), enzyme mix (0.001 μM of PHD2, 10 μM of Fe(II), 100 μM of ascorbate) and peptide mix (0.06 μM of biotinylated C-terminal oxygen dependent degradation domain (CODD) peptide, 2 μM of 2OG) in 50 mM HEPES pH 7.5, 0.01% Tween-20 and 0.1% BSA buffer. Compounds (e.g., IOX2) are preincubated with the enzyme mix for 15 min before being incubated with peptide mix for 10 min at 22°C. Each reaction is quenched with 5 μL of 30 mM EDTA. The bead mix containing AlphaScreen beads is preincubated for 1h with a rabbit monoclonal antibody selective for hydroxy-HIF1α (Pro564) and are added to the wells for a further 1 h at 22°C. The plates are then analyzed with an Envision plate reader. The IC50 values are calculated using nonlinear regression with normalized dose-response fit using Prism GraphPad (n≥3)[1].

Chemical Properties

Molecular Weight	361.22
Formula	C₁₈H₁₄Cl₂N₂O₂
Cas No.	1197300-24-5
Smiles	CN(C(=O)c1c(C)onc1-c1ccccc1Cl)c1ccc(Cl)cc1
Relative Density.	1.346 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 (138.42 mM), Sonication is recommended.

Ethanol: 100 mM, Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (27.68 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7684 mL	13.8420 mL	27.6840 mL	138.4198 mL
5 mM	0.5537 mL	2.7684 mL	5.5368 mL	27.6840 mL
10 mM	0.2768 mL	1.3842 mL	2.7684 mL	13.8420 mL
20 mM	0.1384 mL	0.6921 mL	1.3842 mL	6.9210 mL
50 mM	0.0554 mL	0.2768 mL	0.5537 mL	2.7684 mL
100 mM	0.0277 mL	0.1384 mL	0.2768 mL	1.3842 mL

Calculator

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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