Chemical Name: N,N-Bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-Imidazole-5-methanamine
Biological ActivityNDT 9513727 is a potent C5a receptor (C5aR) negative allosteric modulator (NAM) (IC50 = 11.6 nM); selective for human C5aR (IC50 values for rat and mouse C5aR are > 10 μM). Exhibits inverse agonist pharmacokinetics. Blocks degranulation response in C5a-stimulated U937 cells (IC50 = 7.1 nM). Exhibits selectivity for primate and gerbil receptor over other species. Orally bioavailable.
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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.
Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727.
Citation for NDT 9513727
The citations listed below are publications that use Tocris products. Selected citations for NDT 9513727 include:
1 Citation: Showing 1 - 1
Orthosteric and allosteric action of the C5a receptor antagonists.
Nat Struct Mol Biol 2018;25:472
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