GPBAR-A

Pricing Availability Delivery Time Qty
Cat.No. 4478 - GPBAR-A | C23H15F7N2O2 | CAS No. 877052-79-4
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)
Datasheet
Citations (1)
Literature
Pathways

Biological Activity

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

Compound Libraries

GPBAR-A is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 484.37
Formula C23H15F7N2O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 877052-79-4
PubChem ID 11656002
InChI Key ZIXNJVGTAXRKAP-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 484.37. Batch specific molecular weights may vary from batch to batch due to solvent 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

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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

1 Citation for GPBAR-A

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

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? If so please let us know.

Commented out for usability testing

Reviews

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Literature in this Area

Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling

Pathways for GPBAR-A

Insulin

Insulin Signaling Pathway

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

Protocols

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