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Submit ReviewNIBR 189
Description: Potent and selective EBI2 (GPR183) receptor antagonist
Chemical Name: (2E)-3-(4-Bromophenyl)-1-[4-4-methoxybenzoyl)-1-piperazinyl]-2-propene-1-one
Purity: ≥99% (HPLC)
Biological Activity
Potent and selective EBI2 (GPR183) receptor antagonist (IC50 values are 11 and 15 nM for human and mouse EBI2 receptors respectively). Exhibits selectivity for EBI2 over a panel of other receptors, enzymes and transporters. Blocks oxysterol-induced migration of U937 monocyte cells. Orally bioavailable.
Technical Data
| M. Wt | 429.31 |
| Formula | C21H21BrN2O3 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1599432-08-2 |
| PubChem ID | 36295259 |
| InChI Key | OFHXXBRBGWUOHR-NYYWCZLTSA-N |
| Smiles | BrC1=CC=C(/C=C/C(N2CCN(C(C3=CC=C(OC)C=C3)=O)CC2)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 429.31. 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 | 2.33 mL | 11.65 mL | 23.29 mL |
| 5 mM | 0.47 mL | 2.33 mL | 4.66 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Gessier et al (2014) Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor. J.Med.Chem. 57 3358 PMID: 24678947
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