GPBAR-A | CAS#877052-79-4 | GPBA agonist

MedKoo Cat#: 563019 | Name: GPBAR-A

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GPBAR-A is a synthetic small-molecule agonist of GPBAR1 (G protein-coupled bile acid receptor 1), also known as TGR5. It activates this membrane-bound bile acid receptor, which plays a role in regulating energy homeostasis, glucose metabolism, and immune function. GPBAR-A has been studied for its potential therapeutic applications in metabolic disorders, including type 2 diabetes, obesity, and inflammatory diseases.

Chemical Structure

GPBAR-A

CAS#877052-79-4

Theoretical Analysis

MedKoo Cat#: 563019

Name: GPBAR-A

CAS#: 877052-79-4

Chemical Formula: C23H15F7N2O2

Exact Mass: 484.1022

Molecular Weight: 484.37

Elemental Analysis: C, 57.03; H, 3.12; F, 27.46; N, 5.78; O, 6.61

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	4 Weeks
10mg	USD 650.00	4 Weeks

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Related CAS #

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Synonym

GPBAR-A; GPBAR A; GPBARA;

IUPAC/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

InChi Key

ZIXNJVGTAXRKAP-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H15F7N2O2/c24-19-4-2-1-3-17(19)16-5-6-31-21-18(16)11-32(20(33)12-34-21)10-13-7-14(22(25,26)27)9-15(8-13)23(28,29)30/h1-9H,10-12H2

SMILES Code

O=C1COC2=NC=CC(C3=CC=CC=C3F)=C2CN1CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GPBA receptor (TGR5) agonist.

In vitro activity:

Bile acids and GPBAR-A increased GLP-1 secretion from intestinal cultures, with evidence for synergy between the effects of glucose and GPBA activation. Elevation of cAMP was observed following GPBA activation in individual GLUTag cells. Direct calcium responses to GPBAR-A were small, but in the presence of the agonist, a subpopulation of cells that was previously poorly glucose-responsive exhibited robust glucose responses. Reference: Br J Pharmacol. 2012 Jan;165(2):414-23. https://pubmed.ncbi.nlm.nih.gov/21718300/

In vivo activity:

In vivo, increased delivery of bile to more distal regions of the murine ileum augmented L-cell stimulation. Reference: Br J Pharmacol. 2012 Jan;165(2):414-23. https://pubmed.ncbi.nlm.nih.gov/21718300/

	Solvent	mg/mL	mM
Solubility
	DMSO	48.4	100.00
	Ethanol	9.7	20.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Parker HE, Wallis K, le Roux CW, Wong KY, Reimann F, Gribble FM. Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion. Br J Pharmacol. 2012 Jan;165(2):414-23. doi: 10.1111/j.1476-5381.2011.01561.x. PMID: 21718300; PMCID: PMC3268195.

In vitro protocol:

In vivo protocol:

1: Parker HE, Wallis K, le Roux CW, Wong KY, Reimann F, Gribble FM. Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion. Br J Pharmacol. 2012 Jan;165(2):414-23. doi: 10.1111/j.1476-5381.2011.01561.x. PubMed PMID: 21718300; PubMed Central PMCID: PMC3268195.