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  3. NIBR189

NIBR189 is an EBI2 (Epstein-Barr virus-induced gene 2) antagonist. NIBR189 inhibits human and mouse EBI2 with IC50s of 11 and 16 nM, respectively. NIBR189 can be used for the research of autoimmune diseases.

For research use only. We do not sell to patients.

NIBR189 Chemical Structure

NIBR189 Chemical Structure

CAS No. : 1599432-08-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NIBR189 is an EBI2 (Epstein-Barr virus-induced gene 2) antagonist. NIBR189 inhibits human and mouse EBI2 with IC50s of 11 and 16 nM, respectively. NIBR189 can be used for the research of autoimmune diseases[1].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
11 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
[PMID: 24678947]
CHO IC50
15 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
[PMID: 24678947]
CHO IC50
7 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
[PMID: 24678947]
CHO IC50
8.5 nM
Compound: 4m, NIBR189
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
[PMID: 24678947]
U-937 IC50
0.3 nM
Compound: 4m, NIBR189
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
[PMID: 24678947]
U-937 IC50
9 nM
Compound: 4m, NIBR189
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
[PMID: 24678947]
In Vitro

NIBR189 (0-1 μM; 3 h) blocks migration of U937 cells[1].
NIBR189 (0-10 μM) blocks oxysterol-dependent activation with an IC50 value of 9 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay [1]

Cell Line: U937 cell lines
Concentration: 0-1 μM
Incubation Time: 3 hours
Result: Blocked the direct migration of U937 cells with an IC50 value of 0.3 nM.
In Vivo

1.19 Pharmacokinetic Properties of NIBR189 in Mice[1].

Mice
IV 1 mg/kg
Mice
PO 3 mg/kg
CL (μL/min/mg) 16
t1/2 (h) 1.1
Vss (L/kg) 1.4
AUC (nmol·h/L) 2435 3608
Cmax (nmol/L) 835
tmax (h) 1
F (%) 49

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

429.31

Formula

C21H21BrN2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C(C2=CC=C(OC)C=C2)=O)CC1)/C=C/C3=CC=C(Br)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (116.47 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3293 mL 11.6466 mL 23.2932 mL
5 mM 0.4659 mL 2.3293 mL 4.6586 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3293 mL 11.6466 mL 23.2932 mL 58.2330 mL
5 mM 0.4659 mL 2.3293 mL 4.6586 mL 11.6466 mL
10 mM 0.2329 mL 1.1647 mL 2.3293 mL 5.8233 mL
15 mM 0.1553 mL 0.7764 mL 1.5529 mL 3.8822 mL
20 mM 0.1165 mL 0.5823 mL 1.1647 mL 2.9116 mL
25 mM 0.0932 mL 0.4659 mL 0.9317 mL 2.3293 mL
30 mM 0.0776 mL 0.3882 mL 0.7764 mL 1.9411 mL
40 mM 0.0582 mL 0.2912 mL 0.5823 mL 1.4558 mL
50 mM 0.0466 mL 0.2329 mL 0.4659 mL 1.1647 mL
60 mM 0.0388 mL 0.1941 mL 0.3882 mL 0.9705 mL
80 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.7279 mL
100 mM 0.0233 mL 0.1165 mL 0.2329 mL 0.5823 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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