NIBR189

Catalog No.S0183 Batch:S018301

Technical Data

Formula	C₂₁H₂₁BrN₂O₃
Molecular Weight	429.31	CAS No.	1599432-08-2
Solubility (25°C)*	In vitro	DMSO	21 mg/mL (48.91 mM)
		Ethanol	4 mg/mL (9.31 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

NIBR189, the EBI2 antagonist, blocks the migration of U937 cells expressing functional EBI2 levels with an IC50 of 0.3 nM.^[1]

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models C57BL/6 male mice Dosages 1 mg/kg (i.v.); 3 mg/kg (p.o.) Administration i.v., p.o.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
C57BL/6 male mice
Dosages
1 mg/kg (i.v.); 3 mg/kg (p.o.)
Administration
i.v., p.o.

References

[1] Francois Gessier, et al. J Med Chem. 2014 Apr 24;57(8):3358-68.

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SHIPPING AND STORAGE
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