Pricing Availability   Qty
Description: GPBA receptor (TGR5) agonist
Chemical Name: 4-[[3,5-Bis(trifluoromethyl)phenyl]methyl]-6-(2-fluorophenyl)-4,5-dihydro-pyrido[3,2-f]-1,4-oxazepin-3(2H)-one
Purity: ≥98% (HPLC)
Citations (2)
Pathways (1)

Biological Activity for GPBAR-A

GPBAR-A is a gPBA receptor agonist. Upregulates GLP-1 secretion from intestinal cultures. Increases MQAE-fluorescence suggesting a decrease in intracellular chloride concentration in gallbladder epithelial cells.

Technical Data for GPBAR-A

M. Wt 484.37
Formula C23H15F7N2O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 877052-79-4
PubChem ID 11656002
Smiles O=C(CO3)N(CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)CC1=C3N=CC=C1C2=C(F)C=CC=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GPBAR-A

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 48.44 100
ethanol 9.69 20

Preparing Stock Solutions for GPBAR-A

The following data is based on the product molecular weight 484.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.06 mL 10.32 mL 20.65 mL
5 mM 0.41 mL 2.06 mL 4.13 mL
10 mM 0.21 mL 1.03 mL 2.06 mL
50 mM 0.04 mL 0.21 mL 0.41 mL

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References for GPBAR-A

References are publications that support the biological activity of the product.

Parker et al (2012) Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion. Br.J.Pharmacol. 165 414 PMID: 21718300

Keitel et al (2009) The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders. Hepatology 50 861 PMID: 19582812

If you know of a relevant reference for GPBAR-A, please let us know.

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Keywords: GPBAR-A, GPBAR-A supplier, TGR5, agonists, g-protein, bile, acid, receptors, GPBA, GPBAR, Receptors, 4478, Tocris Bioscience

2 Citations for GPBAR-A

Citations are publications that use Tocris products. Selected citations for GPBAR-A include:

Bas et al (2021) A turquoise fluorescence lifetime-based biosensor for quantitative imaging of intracellular calcium. Nat Commun 12 7159 PMID: 34887382

Kowal et al (2015) Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells. Stem Cells Transl Med 13 28 PMID: 26050734

Do you know of a great paper that uses GPBAR-A from Tocris? Please let us know.

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Pathways for GPBAR-A

Insulin Signaling Pathway

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.