Potent C5a receptor (C5aR) competitive antagonist (IC50
= 11.6 nM); selective for human C5aR (IC50
values for rat and mouse C5aR are > 10 μ
M). Exhibits inverse agonist pharmacokinetics. Blocks degranulation response in C5a-stimulated U937 cells (IC50
= 7.1 nM). Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Identification and characterization of NDT 9513727 [N,N-bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine], a novel, orally bioavailable C5a receptor inverse agonist.
Brodbeck et al.