1. GPCR/G Protein
  2. G protein-coupled Bile Acid Receptor 1
  3. TGR5 Receptor Agonist 3

TGR5 Receptor Agonist 3 

Cat. No.: HY-146453
Handling Instructions

TGR5 Receptor Agonist 3 (Compound 19) is a soft-drug G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.

For research use only. We do not sell to patients.

TGR5 Receptor Agonist 3 Chemical Structure

TGR5 Receptor Agonist 3 Chemical Structure

CAS No. : 2643391-08-4

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Description

TGR5 Receptor Agonist 3 (Compound 19) is a soft-drug G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively[1].

In Vitro

TGR5 Receptor Agonist 3 (compound 19) (10-50μM, 2 hours) activates TGR5 in fetal rat intestinal cells (FRIC) and NCI-H716 cells to promote GLP-1 secretion in a dose-dependent manner[1].

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

In Vivo

TGR5 Receptor Agonist 3 (compound 19) has good targeting and can effectively activate TGR5, thus promoting the secretion of GLP-1 in plasma and regulating the homeostasis of glucose metabolism in male ICR mice[1].
TGR5 Receptor Agonist 3 (compound 19) can be rapidly absorbed and metabolized in male ICR mice, and has a good safety profile[1].
TGR5 Receptor Agonist 3 (compound 19) (oral gavage; 50 mg/kg; one hour) can be gavaged into overnight-fasted male ICR mice for one hour with a Cmaxvalue of 0.003 μg/mL [1].
TGR5 Receptor Agonist 3 (compound 19) can reduce gallbladder-filling and safety in vivo[1].

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

Molecular Weight

513.54

Formula

C29H27N3O6

CAS No.
SMILES

CCOCOC(C1=COC2=C1C=C(C=C2)OC3=C(C=NC=C3)C(N4CCN(C5=C4C=CC=C5)C6CC6)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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TGR5 Receptor Agonist 3
Cat. No.:
HY-146453
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