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NIBR189

Cat. No. M6141
NIBR189 Structure
Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 165  USD165 In stock
50mg USD 540  USD540 In stock
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Quality Control & Documentation
Biological Activity

The effects of oxysterols on macrophage migration have been shown to be partially inhibited with EBI2 antagonist (NIBR189) indicating EBI2 mediated signalling. EBI2 antagonist NIBR189 inhibited the effects of 7α25HC on macrophage migration, that was exogenously applied to the lower chamber of the xCELLigence® migration transwell system. Importantly, conditioned media taken from astrocytes stimulated with LPS for 6 and 8 hours (LPS-Astro-Med) and supplemented with EBI2 antagonist (NIBR189) attenuated the observed macrophage migration.

Protocol (for reference only)
Cell Experiment
Cell lines RAW264.7 cell
Preparation method The migration of cells through the electrode array from the upper to lower chambers is measured by an increase in impedance. The bottom chamber of the plate was filled with either astrocyte conditioned media or serum free media supplemented with 7α25HC (0.01 μM) with or without EBI2 antagonist NIBR189 (10 μM). Cell migration was recorded immediately after the plate was re-inserted and recorded for 2 hours.
Concentrations 10 μM
Incubation time 2 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 429.31
Formula C21H21BrN2O3
CAS Number 1599432-08-2
Solubility (25°C) 47 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rutkowska A, et al. Sci Rep. The EBI2 signalling pathway plays a role in cellular crosstalk between astrocytes and macrophages.

[2] Gessier F, et al. J Med Chem. Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor.

[3]

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