產品描述: NIBR189 是 Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor 的有效拮抗劑,其結合的IC50值為16 nM,其功能的IC50值為11 nM |
靶點:
EBI2 (function)(Cell-free assay):11 nM; EBI2 (binding)(Cell-free assay):16 nM;EBI2/GPR183 |
體外研究:
NIBR189, the EBI2 antagonist, blocks the migration of U937 cells expressing functional EBI2 levels with an IC50 of 0.3 nM |
體內研究:
NIBR189 is a potent and selective EBI2 antagonist with pharmacokinetic properties which should allow use for in vitro and in vivo experiments |
細胞實驗:
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. |
動物實驗:
Animal Models: C57BL/6 male mice Dosages: 1 mg/kg (i.v.); 3 mg/kg (p.o.) Administration: i.v., p.o. |
參考文獻:
1. Francois Gessier, et al. Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor. J Med Chem. 2014 Apr 24;57(8):3358-68. |
溶解性:
Soluble in DMSO、Ethanol |
保存條件:
-20℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
2.329 ml |
11.647 ml |
23.293 ml |
5 mM |
0.466 ml |
2.329 ml |
4.659 ml |
10 mM |
0.233 ml |
1.165 ml |
2.329 ml |
50 mM |
0.047 ml |
0.233 ml |
0.466 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |