Shopping Cart

Remove All

Your shopping cart is currently empty

Proceed to checkout Continue shopping

TGR5 agonist 10

Name: TGR5 agonist 10
Brand: TargetMol
SKU: T218011
Rating: 4.5 (1 reviews)

Copy Product Info

🥰Excellent

Synonyms:

Catalog No. T218011 Copy Product Info

🥰Excellent

TGR5 agonist 10 is a selective, allosteric, and orally bioavailable agonist for the Takeda G protein-coupled receptor 5 (TGR5), with EC50 values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. It demonstrates specificity for TGR5 over FXR and can activate both human and mouse TGR5 to induce cAMP accumulation. The compound enhances cholic acid's functional activity and efficacy on hTGR5 and shows higher selectivity in cAMP formation compared to β-arrestin 2 recruitment. TGR5 agonist 10 exhibits hypoglycemic effects in an oral glucose tolerance test in Mus musculus and can be utilized in diabetes research.

Cas No. 3081614-92-5

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

Add to Quotation

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

Questions

Resource Download

Product Introduction

Bioactivity

Description	TGR5 agonist 10 is a selective, allosteric, and orally bioavailable agonist for the Takeda G protein-coupled receptor 5 (TGR5), with EC50 values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. It demonstrates specificity for TGR5 over FXR and can activate both human and mouse TGR5 to induce cAMP accumulation. The compound enhances cholic acid's functional activity and efficacy on hTGR5 and shows higher selectivity in cAMP formation compared to β-arrestin 2 recruitment. TGR5 agonist 10 exhibits hypoglycemic effects in an oral glucose tolerance test in Mus musculus and can be utilized in diabetes research.
Targets & IC50	TGR5 (human):0.8 μM (EC50)
In vitro	TGR5 agonist 10 (compound A1) demonstrates low activity in recruiting β-arrestin2 (EC50 = 26.5 μM), which is weaker than its activity in cAMP accumulation in HEK293T cells. When tested at concentrations of 10 μM or 20 μM over 8 hours in HEK293T cells, it does not activate FXR, indicating selectivity for TGR5.
In vivo	Compound A1, a TGR5 agonist, demonstrates a significant glucose-lowering effect in the OGTT model with ICR mice when administered at 100 mg/kg via oral gavage.

Chemical Properties

Molecular Weight	436.58
Formula	C₂₅H₄₀O₆
Cas No.	3081614-92-5
Smiles	O(C)[C@H]1[C@]2([C@]3([C@@](C)([C@@]([C@@H](CCC(O)=O)C)(CC3)[H])OC(=O)C[C@@]2([C@]4(C)[C@](C1)(C[C@H](O)CC4)[H])[H])[H])[H]

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.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

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

Related Tags: TGR5 agonist 10 chemical structure | TGR5 agonist 10 in vivo | TGR5 agonist 10 in vitro | TGR5 agonist 10 formula | TGR5 agonist 10 molecular weight