Home GPCR & G Protein GPR antagonist NIBR189 For research use only.

NIBR189

NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.

NIBR189 Chemical Structure

NIBR189 Chemical Structure

CAS No. 1599432-08-2

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NIBR189 Related Products

Biological Activity

Description NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
Targets
EBI2 (function) [1]
(Cell-free assay)		 EBI2 (binding) [1]
(Cell-free assay)
11 nM 16 nM
In vitro
In vitro

NIBR189, the EBI2 antagonist, blocks the migration of U937 cells expressing functional EBI2 levels with an IC50 of 0.3 nM.[1]
Cell Research Cell lines U937 cells
Concentrations 20 nM
Incubation Time 3 h
Method

Prior to the migration assay, U937 cells were kept overnight in lipid-depleted media. Chemotaxis was performed using HTS Transwell-96 plates with 5.0 μm pore polycarbonate membranes. In brief, lower chambers were filled with 240 μL of compound solution in media in which the FCS was substituted with 1% BSA, and after insertion of the filters, 0.75×105 cells in 75 μL media were added to the upper chamber. After 3 h at 37℃, cells in the lower chamber were analyzed by flow cytometry.
In Vivo
In vivo

NIBR189 is a potent and selective EBI2 antagonist with pharmacokinetic properties which should allow use for in vitro and in vivo experiments.[1]
Animal Research Animal Models C57BL/6 male mice
Dosages 1 mg/kg (i.v.); 3 mg/kg (p.o.)
Administration i.v., p.o.

Chemical Information & Solubility

Molecular Weight 429.31 Formula

C21H21BrN2O3
CAS No. 1599432-08-2 SDF --
Smiles COC1=CC=C(C=C1)C(=O)N2CCN(CC2)C(=O)C=CC3=CC=C(C=C3)Br
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 21 mg/mL ( (48.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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